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Drug Discovery Program

Laboratory projects include structural studies of biological macromolecules, structure-function relationship of lypases and molecular modeling application on medicinal subjects.

Program Details | Biography Details | Publications

  DRUG DISCOVERY PROGRAM

PROGRAM DETAILS

Research areas include: chemical studies on beta-lactam antibiotics; total synthesis and structure determination of biologically active natural products; synthesis of pyrimidine derivatives as antiviral and antitumor agents. The following methodologies have been used in such studies: classical methodologies for organic synthesis, methodologies for the solid phase synthesis of small molecules, use of enzymes, microwave, and parallel synthesis. Prof. Botta’s team is involved in structural studies of biological macromolecules (enzymes, receptors, growth factors), studies about structure-function relationship of lypases, molecular modeling application on medicinal subjects. Moreover, in recent years he started to work on Virtual Library Design and Virtual Screening.

  DRUG DISCOVERY PROGRAM

BIOGRAPHY DETAILS

Maurizio Botta, Ph.D.
Adjunct Professor at Temple University
Director, Drug Discovery Program
Professor of Medicinal Chemistry at the University of Siena

Prof. Maurizio Botta, Ph.D. (U.N.B. – Canada) is full Professor of Medicinal Chemistry at the Faculty of Pharmacy, University of Siena and, from Adjunct Professor in Temple University’s college of Science and Technology, in the Department of Biology, Philadelphia (USA). Since November 2002 he is Head of the Dipartimento Farmaco Chimico Tecnologico of the same University.

Prof. Botta serves as the EU expert for reviewing projects belonging to the TMR research program, for the mid-term review of the approved TMR projects. He is Executive Guest Editor of “Current Pharmaceutical Design” in the field of Anti-Angiogenesis Agents, EU expert in the panel “Quality of Life” for reviewing projects belonging to the “Life sciences, genomics and biotechnology for health” research program. He serves as projects reviewer for Italian and Slovenian Research Projects, for the Austrian Research Fund (Wissenschaftsfonds-FWF), for the Cancer Research UK Programme and for “Fondazione Roma” and for the French National Research Agency.

Prof. Botta is a Member of the Advisory Editorial Board for “ChemMedChem” (Wiley) and for the “Journal of Medicinal Chemistry” (ACS).

Prof. Botta has been a memberof the “Società Chimica Italiana” since 1976, a member of the American Chemical Society since 1984 and of the QSAR Society since 1997. From 1998 to 2004, he was member of the “Direttivo della Divisione di Chimica Farmaceutica della Società Chimica Italiana”. He was Chairman of 18 scientific schools and meetings, among which Schools of Synthetic Methodologies in Medicinal Chemistry of SCI and European Workshops in Drug Design and in Drug Synthesis, of the “Twelfth FeCheM – conference on Heterocycles in Bio-Organic Chemistry”, held at University of Siena; he was co-Chairman at the Conference “3rd IUPAC-2002 International Symposium on the Chemistry of Natural Products” in Firenze. Since 1998, he has contributed to the organization of more than 80 scientific seminars at the Dipartimento Farmaco Chimico Tecnologico of Siena University.

He carries out reviewing activities for well- known journals in organic and medicinal chemistry, and has received five Merck Research Laboratories Awards for "Academic Development Programs in Chemistry" (1996, 1997, 1998, 2001, and 2002). Since 1988 his research has been supported by the University of Siena, MIUR, CNR, EU, and pharmaceutical companies.

Professor Botta has authored 253 papers, and holds 14 patents on his discoveries.

  DRUG DISCOVERY PROGRAM

SELECTED PUBLICATIONS

1) C. TINTORI, M. MAGNANI, S. SCHENONE, M. BOTTA - 'Docking, 3D-QSAR studies and in silico ADME prediction on c-Src tyrosine kinase inhibitors ' (pubblicazione su rivista, 2008) EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY; in corso di stampa (lettera di accettazione del 03-07-2008)

2) F. MANETTI, F. FALCHI, E. CRESPAN, S. SCHENONE, G. MAGA, M. BOTTA - 'N-(thiazol-2-yl)-2-thiophene carboxamide derivatives as Abl inhibitors identified by a pharmacophore-based database screening of commercially available compounds ' (pubblicazione su rivista, 2008) BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, Vol.18, 4328 - 4331

3) M. BIAVA, G. C. PORRETTA, G. POCE, A. DE LOGU, M. SADDI, R. MELEDDU, F. MANETTI, E. DE ROSSI, M. BOTTA - '1,5-Diphenylpyrrole Derivatives as Antimycobacterial Agents. Probing the Influence on Antimycobacterial Activity of Lipophilic Substituents at the Phenyl Rings ' (pubblicazione su rivista, 2008) JOURNAL OF MEDICINAL CHEMISTRY, Vol.51, 3644 - 3648

4) M. RADI, C. FALCIANI, L. CONTEMORI, E. PETRICCI, G. MAGA, A. SAMUELE, S. ZANOLI, M. TERRAZAS, M. CASTRIA, A. TOGNINELLI, J. A. ESTÉ, I. CLOTET-CODINA, M. ARMAND-UGON, M. BOTTA - 'A Multidisciplinary Approach for the Identification ofNovel HIV-1 Non-Nucleoside Reverse TranscriptaseInhibitors: S-DABOCs and DAVPs ' (pubblicazione su rivista, 2008) chemmedchem; in corso di stampa (lettera di accettazione del 27-08-2007)

5) M. RADI, S. SALETTI, M. BOTTA - 'A one-pot, two step microwave-assisted synthesis of highly functionalized benzoxazoles using solid-supported reagents (SSRs) ' (pubblicazione su rivista, 2008) TETRAHEDRON LETTERS, Vol.49, 4464 - 4466

6) A. SPREAFICO, S. SCHENONE, T. SERCHI, M. ORLANDINI, A. ANGELUCCI, D. MAGRINI, G. BERNARDINI, G. COLLODEL, A. DI STEFANO, C. TINTORI, M. BOLOGNA, F. MANETTI, M. BOTTA, A. SANTUCCI - 'Antiproliferative and proapoptotic activities of new pyrazolo[3,4-d]pyrimidine derivative Src kinase inhibitors in human osteosarcoma cells ' (pubblicazione su rivista, 2008) FASEB JOURNAL, Vol.22, 1560 - 1571

7) M. CELANO, S. SCHENONE, D. COSCO, M. NAVARRA, E. PUXEDDU, L. RACANICCHI, C. BRULLO, E. VARANO, S. ALCARO, E. FERRETTI, G. BOTTA, S. FILETTI, M. FRESTA, M. BOTTA, D. RUSSO - 'Cytotoxic effects of a novel pyrazolopyrimidine derivative entrapped in liposomes in anaplastic thyroid cancer cells in vitro and in xenograft tumors in vivo ' (pubblicazione su rivista, 2008) ENDOCRINE-RELATED CANCER, Vol.15, 499 - 510

8) M. RADI, E. CRESPAN, G. BOTTA, F. FALCHI, G. MAGA, F. MANETTI, V. CORRADI, M. MANCINI, M. A. SANTUCCI, S. SCHENONE, M. BOTTA - 'Discovery and SAR of 1,3,4-thiadiazole derivatives as potent Abl Tyrosine Kinase inhibitors and cytodifferentiating agents ' (pubblicazione su rivista, 2008) BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, Vol.18, 1207 - 1211

9) R. ANGELINI, A. TISI, G. REA, M. M. CHEN, M. BOTTA, R. FEDERICO, A. CONA - 'Involvement of Polyamine Oxidase in Wound Healing 1,2[W] ' (pubblicazione su rivista, 2008) PLANT PHYSIOLOGY, Vol.146, 162 - 177

10) B. BOTTA, A. TAFI, F. CAPORUSCIO, M. BOTTA, L. NEVOLA, I. D'ACQUARICA, C. FRASCHETTI, M. SPERANZA - 'Modelling Amphetamine/Receptor Interactions: A Gas-Phase Study of Complexes Formed between Amphetamine and Some Chiral Amido[4]resorcinarenes ' (pubblicazione su rivista, 2008) CHEMISTRY A EUROPEAN JOURNAL , Vol.14, 3585 - 3595

11) E. TASSONI, F. GIANNESSI, T. BRUNETTI, P. PESSOTTO, M. L. RENZULLI, M. TRAVAGLI, S. RAJAMAKI, S. PRATI, S. DOTTORI, F. CORELLI, W. CABRI, P. CARMINATI, M. BOTTA - 'Novel Substituted Aminoalkylguanidines as Potential Antihyperglycemic and Food Intake-Reducing Agents ' (pubblicazione su rivista, 2008) J. Med. Chem. , Vol.51, 3073 - 3076

12) D. GROHMANN, V. CORRADI, M. ELBASYOUNY, A. BAUDE, F. HORENKAMP, S. D. LAUFER, F. MANETTI, M. BOTTA, T. RESTLE - 'Small Molecule Inhibitors Targeting HIV-1 Reverse Transcriptase Dimerization ' (pubblicazione su rivista, 2008) Chembiochem, Vol.9, 916 - 922

13) F. MANETTI, C. BRULLO, M. MAGNANI, F. MOSCI, B. CHELLI, E. CRESPAN, S. SCHENONE, A. NALDINI, O. BRUNO, M. . L. TRINCAVELLI, G. MAGA, F. CARRARO, C. MARTINI, F. BONDAVALLI, M. BOTTA - 'Structure-Based Optimization of Pyrazolo[3,4-d]pyrimidines as Abl Inhibitors and Antiproliferative Agents toward Human Leukemia Cell Lines. ' (pubblicazione su rivista, 2008) J Med Chem, Vol.51, 1252 - 1259

14) T. TUCCINARDI , S. SCHENONE, F. BONDAVALLI, C. BRULLO, O. BRUNO, L. MOSTI, A. ZIZZARI, C. TINTORI, F. MANETTI, O. CIAMPI, M. . L. TRINCAVELLI, C. MARTINI, A. MARTINELLI, M. BOTTA - 'Substituted Pyrazolo[3,4-b]pyridines as Potent A1 Adenosine Antagonists: Synthesis, Biological Evaluation, and Development of an A1 Bovine Receptor Model ' (pubblicazione su rivista, 2008) chemmedchem, Vol.3, 898 - 913

15) S. AVRAMOVA, E. GALLETTI, M. RENZULLI, G. GIORGI, G. SGARAGLI, D. ALDERIGHI, C. GHIRON, F. CORELLI, M. RADI, M. BOTTA - 'Synthesis of an Original Oxygenated Taxuspine X Analogue: a Versatile "Non-Natural" Natural Product with Remarkable P-gp Modulating Activity ' (pubblicazione su rivista, 2008) chemmedchem, Vol.3, 745 - 748

16) M. ANZINI, M. ROVINI, A. CAPPELLI, S. VOMERO, F. MANETTI, M. BOTTA, L. SAUTEBIN, A. ROSSI, C. GHELARDINI, M. NORCINI, F. MAKOVEC, P. ANZELLOTTI, P. PATRIGNANI, M. BIAVA - 'Synthesis, Biological Evaluation, and Enzyme Docking Simulations of 1,5-Diarylpyrrole-3-Alkoxyethyl Ethers as Selective Cyclooxygenase-2 Inhibitors Endowed with Anti-inflammatory and Antinociceptive Activity ' (pubblicazione su rivista, 2008) J. Med. Chem. ; in corso di stampa (lettera di accettazione del 19-05-2008)

17) R. SILVESTRI, M. G. CASCIO , G. LA REGINA, G. PISCITELLI, G. LAVECCHIA, A. BRIZZI, S. PASQUINI, M. BOTTA, E. NOVELLINO, V. DI MARZO, F. CORELLI - 'Synthesis, Cannabinoid Receptor Affinity, and Molecular Modeling Studies of Substituted 1-Aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides. ' (pubblicazione su rivista, 2008) JOURNAL OF MEDICINAL CHEMISTRY, Vol.51, 1560 - 1576

18) M. RADI, L. CONTEMORI, D. CASTAGNOLO, R. SPINOSA, J. A. ESTE', S. MASSA, M. BOTTA - ' A Versatile Route to C-6 Arylmethyl-Functionalized S-DABO and Related Analogues ' (pubblicazione su rivista, 2007) ORGANIC LETTERS, Vol.9, 3157 - 3160

19) C. PALOCCI, M. FALCONI, S. ALCARO, A. TAFI, R. PUGLISI, F. ORTUSO, M. BOTTA, L. ALBERGHINA , E. CERNIA - 'An approach to address Candida rugosa lipase regioselectivity in the acylation reactions of trytilated glucosides ' (pubblicazione su rivista, 2007) JOURNAL OF BIOTECHNOLOGY, Vol.128, 908 - 918

20) E. DREASSI, A. ZIZZARI, S. D'AREZZO, P. VISCA, M. BOTTA - 'Analysis of guazatine mixture by Lc and LC-MS and antimycotic activity determination of principal components' (pubblicazione su rivista, 2007) JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, Vol.43, 1499 - 1506

21) S. SCHENONE, BONDAVALLI F., M. BOTTA - 'Antiangiogenic Agents: an update on small molecule VEGFR inhibitors ' (pubblicazione su rivista, 2007) CURRENT MEDICINAL CHEMISTRY, Vol.14, 2495 - 2516

22) T. TUCCINARDI, F. MANETTI, S. SCHENONE, A. MARTINELLI, M. BOTTA - 'Construction and Validation of a RET TK Catalytic Domain by Homology Modeling' (pubblicazione su rivista, 2007) journal of chemical information and modeling, Vol.47, 644 - 655

23) M. BIAVA, G. C. PORRETTA, G. POCE, S. SUPINO, S. FORLI, M. ROVINI, A. CAPPELLI, F. MANETTI, M. BOTTA, L. SAUTEBIN, A. ROSSI, C. PERGOLA, C. GHELARDINI, E. VIVOLI, F. MAKOVEC, P. ANZELLOTTI, P. PATRIGNANI, M. ANZINI - 'Cyclooxygenase-2 Inhibitors. 1,5-Diarylpyrrol-3-acetic Esters with Enhanced Inhibitory Activity Toward Cyclooxygenase-2 and Improved Cyclooxygenase-2/Cyclooxygenase-1 Selectivity' (pubblicazione su rivista, 2007) JOURNAL OF MEDICINAL CHEMISTRY, Vol.50, 5403 - 5411

24) C. MUGNAINI, M. ALONGI, A. TOGNINELLI, H. GEVARIYA, A. BRIZZI, F. MANETTI, C. BERNARDINI, L. ANGELI, A. TAFI, L. BELLUCCI, F. CORELLI, S. MASSA, G. MAGA, A. SAMUELE, M. FACCHINI, I. CLOTET-CODINA, M. ARMAND-UGON, J. A. ESTE, M. BOTTA - 'Dihydro-alkylthio-benzyl-oxopyrimidines as Inhibitors of Reverse Transcriptase: Synthesis and Rationalization of the Biological Data on Both Wild-Type Enzyme and Relevant Clinical Mutants ' (pubblicazione su rivista, 2007) JOURNAL OF MEDICINAL CHEMISTRY, Vol.50, 6580 - 6595

25) G. MAGA, M. RADI, S. ZANOLI, F. MANETTI, R. CANCIO, U. HUBSCHER, S. SPADARI, C. FALCIANI, M. TERRAZAS, J. VILARRASA, M. BOTTA - 'Discovery of Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase (RT) Competing with the Nucleotide Substrate' (pubblicazione su rivista, 2007) Angew.Chem.Int.Ed., Vol.46, 1810 - 1813

26) F. RAFFI, F. CORELLI, M. BOTTA - 'Efficient synthesis of iminoctadine, a potent antifungal agent and polyamine oxidase inhibitor (PAO)' (pubblicazione su rivista, 2007) SYNTHESIS, Vol.xx, 3013 - 3016

27) R. MORISI, M. CELANO, E. TOSI, S. SCHENONE, M. NAVARRA, E. FERRETTI, G. COSTANTE, C. DURANTE, G. BOTTA, M. D'AGOSTINO, C. BRULLO, S. FILETTI, M. BOTTA, D. RUSSO - 'Growth inhibition of medullary thyroid carcinoma cells by pyrazolo-pyrimidine derivatives ' (pubblicazione su rivista, 2007) JOURNAL OF ENDOCRINOLOGICAL INVESTIGATION, Vol.30, 31 - 31

28) F. MANETTI, A. SANTUCCI, G. A. LOCATELLI, G. MAGA, A. SPREAFICO, T. SERCHI, M. ORLANDINI, G. BERNARDINI, N. P. CARADONNA, A. SPALLAROSSA, C. BRULLO, S. SCHENONE, O. BRUNO, A. RANISE, F. BONDAVALLI, O. HOFFMANN, M. BOLOGNA, A. ANGELUCCI, M. BOTTA - 'Identification of a novel pyrazolo[3,4-d]pyrimidine able to inhibit cell proliferation of a human osteogenic sarcoma in vitro and in a xenograft model in mice' (pubblicazione su rivista, 2007) JOURNAL OF MEDICINAL CHEMISTRY, Vol.50, 5579 - 5588

29) F. MANETTI, A. PUCCI, M. MAGNANI, G. A. LOCATELLI, C. BRULLO, A. NALDINI, S. SCHENONE, G. MAGA, F. CARRARO, M. BOTTA - 'Inhibition of Bcr-Abl Phosphorylation and Induction of Apoptosis by Pyrazolo[3,4-d]pyrimidines in Human Leukemia Cells ' (pubblicazione su rivista, 2007) chemmedchem, Vol.2, 343 - 353

30) E. DREASSI, A. ZIZZARI, A. ZANFINI, G. CORBINI, M. BOTTA - 'LC/ESI/MS METHOD FOR THE QUANTITATIVE DETECTION OF GUAZATINE RESIDUES IN CEREALS' (pubblicazione su rivista, 2007) J Agric Food Chem, Vol.55, 6850 - 6856

31) S. SCHENONE, F. MANETTI, M. BOTTA - 'Last findings on dual inhibitors of Abl and Src tyrosine-kinases' (pubblicazione su rivista, 2007) Mini-Reviews in Medicinal Chemistry, Vol.7, 191 - 201

32) C. TINTORI, F. MANETTI, N. VELJKOVIC, V. PEROVIC, J. VERCAMMEN, S. HAYES, S. MASSA, M. WITVROUW, Z. DEBYSER, V. VELJKOVIC, M. BOTTA - 'Novel Virtual Screening Protocol Based on the Combined Use of Molecular Modeling and Electron-Ion Interaction Potential Techniques To Design HIV-1 Integrase Inhibitors' (pubblicazione su rivista, 2007) journal of chemical information and modeling, Vol.47, 1536 - 1544

33) E. RAIBER, J. A. WILKINSON, F. MANETTI, M. BOTTA, J. DEAKIN, J. GALLAGHER, M. LYON, S. W. DUCKI - 'Novel heparin/heparan sulfate mimics as inhibitors of HGF/SF-induced MET activation' (pubblicazione su rivista, 2007) BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, Vol.17, 6321 - 6325

34) E. GALLETTI, M. MAGNANI, M. RENZULLI, M. BOTTA - 'Paclitaxel and Docetaxel Resistance: Molecular Mechanism and Development of new generation Taxanes ' (pubblicazione su rivista, 2007) Chem Med Chem , Vol.2, 920 - 942

35) D. CASTAGNOLO, G. GIORGI, R. SPINOSA, F. CORELLI, M. BOTTA - 'Practical syntheses of enantiomerically pure N-acetylbenzhydrylamines ' (pubblicazione su rivista, 2007) EUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Vol.-, 3676 - 3686

36) S. DONNINI, M. MONTI, C. CASTAGNINI , R. SOLITO, M. BOTTA, A. GIACHETTI, M. ZICHE - 'Pyrazolo-pyrimidine-derived c-Src inhibitor reduces angiogenesis and survival of squamous carcinoma cells by suppressing vascular endothelial growth factor production and signaling.' (pubblicazione su rivista, 2007) INTERNATIONAL JOURNAL OF CANCER, Vol.120, 995 - 1004

37) S. SCHENONE, F. MANETTI, M. BOTTA - 'Src Inhibitors and Angiogenesis' (pubblicazione su rivista, 2007) CURRENT PHARMACEUTICAL DESIGN, Vol.13, 2118 - 2128

38) M. RADI, E. PETRICCI, F. CORELLI, M. BOTTA - 'Stereoselective synthesis of N1-6-methyluridine and related 2-substituted analogues.' (pubblicazione su rivista, 2007) HETEROCYCLES, Vol.72, 79 - 83

39) E. GALLETTI, S. I. AVRAMOVA, M. L. RENZULLI, F. CORELLI, M. BOTTA - 'Stereoselective synthesis of advanced intermediates en route to Taxuspine U and X: a study of macrocyclization via ring closing metathesis to highly constrained twelve-membered rings.' (pubblicazione su rivista, 2007) TETRAHEDRON LETTERS, Vol.48, 751 - 754

40) M. L. RENZULLI, L. ROCHEBLAVE, S. I. AVRAMOVA, E. GALLETTI, D. CASTAGNOLO, A. TAFI, F. CORELLI, M. BOTTA - 'Studies towards the synthesis of the bicyclic 3,8-secotaxane diterpenoid system using a ring closing metathesis strategy' (pubblicazione su rivista, 2007) TETRAHEDRON, Vol.63, 497 - 509

41) M. BOTTA, S. ARMAROLI, D. CASTAGNOLO, G. FONTANA, P. PERA, E. BOMBARDELLI - 'Synthesis and Biological Evaluation of New Taxoids Derived from 2-Deacetoxytaxinine J' (pubblicazione su rivista, 2007) Bioorganic Medicinal Chemistry Letters, 17 (2007), 1579 - 1583

42) C. MUGNAINI, E. PETRICCI, M. BOTTA, F. CORELLI, P. MASTROMARINO, G. GIORGI - 'Synthesis and biological evaluation of 4-alkylamino-6-(2-hydroxyethyl)-2-methylthiopyrimidines as new rubella virus inhibitors' (pubblicazione su rivista, 2007) EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, Vol.42, 256 - 262

43) D. CASTAGNOLO, F. DESSI, M. RADI, M. BOTTA - 'Synthesis of enantiomerically pure α-[4-(1-substituted)-1,2,3-triazol-4-yl]-benzylacetamides via microwave-assisted click chemistry: towards new potential antimicrobial agents' (pubblicazione su rivista, 2007) Tetrahedron Asymmetry, Vol.18, 1345 - 1350

44) S. SCHENONE, F. MANETTI, M. BOTTA - 'Synthetic Src-kinase domain inhibitors and their structural requirements' (pubblicazione su rivista, 2007) Anti-Cancer Agents in Medicinal Chemistry, Vol.7, 660 - 680

45) C. MUGNAINI, S. RAJAMAKI, C. TINTORI, F. CORELLI, S. MASSA, M. WITVROUW, Z. DEBYSER, V. VELJKOVIC, M. BOTTA - 'Toward novel HIV-1 integrase binding inhibitors: Molecular modeling, synthesis, and biological studies.' (pubblicazione su rivista, 2007) BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, Vol.17, 5370 - 5373

46) F. MANETTI, C. TINTORI, M. ARMAND-UGON, I. CLOTET-CODINA, S. MASSA, R. RAGNO, J. A. ESTE, M. BOTTA - 'A Combination of Molecular Dynamics and Docking Calculations to Explore the Binding Mode of ADS-J1, a Polyanionic Compound Endowed with Anti-HIV-1 Activity' (pubblicazione su rivista, 2006) journal of chemical information and modeling, Vol.46, 1344 - 1351

47) L. MACCARI, M. MAGNANI, G. STRAPPAGHETTI, F. CORELLI, M. BOTTA, F. MANETTI - 'A GFA-based QSAR model for the affinity of arylpiperazines toward a1 adrenoceptors.' (pubblicazione su rivista, 2006) journal of chemical information and modeling, Vol.46, 1466 - 1478

48) F. MANETTI, G. A. LOCATELLI, G. MAGA, S. SCHENONE, M. MODUGNO, S. FORLI, F. CORELLI, M. BOTTA - 'A combination of docking/dynamics simulations and pharmacophoric modeling to discover new dual c-Src/Abl kinase inhibitors' (pubblicazione su rivista, 2006) JOURNAL OF MEDICINAL CHEMISTRY, Vol.49, 3278 - 3286

49) M. RENZULLI, L. ROCHEBLAVE, S. I. AVRAMOVA, E. GALLETTI, D. CASTAGNOLO, L. MACCARI, S. FORLI, F. MANETTI, F. CORELLI, M. BOTTA - 'A pharmacophore modeling approach to design new taxol® mimics: towards the synthesis of potential anticancer and MDR-reversing agent' (pubblicazione su rivista, 2006) ARKIVOC, Vol.viii, 111 - 130

50) M. BIAVA, G. C. PORRETTA, G. POCE, S. SUPINO, D. DEIDDA, R. POMPEI, P. MOLICOTTI, F. MANETTI, M. BOTTA - 'Antimycobacterial Agents. Novel Diarylpyrrole Derivatives of BM212 Endowed with High Activity toward Mycobacterium tuberculosis and Low Cytotoxicity' (pubblicazione su rivista, 2006) JOURNAL OF MEDICINAL CHEMISTRY, Vol.49, 4946 - 4952

51) F. MANETTI, M. BOTTA, A. TAFI - 'Application of pharmacophore models in medicinal chemistry' (pubblicazione su volume collettaneo, 2006) , 253 - 282 Volume: Pharmacophores and Pharmacophore Searches, Casa Editrice: Wiley-VCH (GERMANIA), Weinheim, Germania

52) A. TAFI, L. ANGELI, VENTURINI, TRAVAGLI, F. CORELLI, M. BOTTA - 'Computational studies of competitive inhibitors of nitric oxide synthase (NOS) enzymes: towards the development of powerful and isoform-selective inhibitors.' (pubblicazione su rivista, 2006) CURRENT MEDICINAL CHEMISTRY, Vol.13, 1929 - 1946

53) M. RADI, R. SPINOSA, M. C. PARLATO, F. CORELLI, M. BOTTA - 'Exploring the Synthesis of Masked Phosphoramido 6-Vinylcytidine Derivatives as Building Blocks for Cross-Linking Oligonucleotides ' (pubblicazione su rivista, 2006) HETEROCYCLES, Vol.69, 151 - 166

54) B. BOTTA, F. CAPORUSCIO, D. SUBISSATI, A. TAFI, M. BOTTA, A. FILIPPI, M. SPERANZA - 'Flattened Cone 2,8,14,20-Tetrakis (L-valinamido)[4]resorcinarene: An Enantioselective Allosteric Receptor in the Gas Phase' (pubblicazione su rivista, 2006) Angewandte Chemie, Vol.45, 2717 - 2720

55) A. CONA, G. REA, M. BOTTA, F. CORELLI, R. FEDERICO, R. ANGELINI - 'Flavin-containing polyamine oxidase is a hydrogen peroxide source in the oxidative response to the protein phosphatase inhibitor cantharidin in Zea mays L.' (pubblicazione su rivista, 2006) JOURNAL OF EXPERIMENTAL BOTANY, Vol.57, 2277 - 2289

56) B. BOTTA, F. CAPORUSCIO, I. D'ACQUARICA, G. DELLE MONACHE, D. SUBISSATI, A. TAFI, M. BOTTA, A. FILIPPI, M. SPERANZA - 'Gas-Phase Enantioselectivity of Chiral Amido[4]resorcinarene Receptors' (pubblicazione su rivista, 2006) CHEMISTRY-A EUROPEAN JOURNAL, Vol.10, 04126 - 4135

57) M. BIANCHI, F. POLTICELLI, P. ASCENZI, M. BOTTA, R. FEDERICO, P. MARIOTTINI, A. CONA - 'Inhibition of polyamine and spermine oxidases by polyamine analogues' (pubblicazione su rivista, 2006) The FEBS Journal, Vol.273, 1115 - 1123

58) F. MANETTI, M. MAGNANI, D. CASTAGNOLO, L. PASSALACQUA, M. BOTTA, F. CORELLI, M. SADDI, D. DEIDDA, A. DE LOGU - 'Ligand-Based Virtual Screening, Parallel Solution-Phase and Microwave-Assisted Synthesis as Tools to Identify and Synthesize New Inhibitors of Mycobacterium tuberculosis' (pubblicazione su rivista, 2006) chemmedchem, Vol.1, 973 - 989

59) A. TAFI, C. BERNARDINI, M. BOTTA, F. CORELLI, M. ANDREINI, A. MARTINELLI, G. ORTORE, P. BARALDI, F. FRUTTAROLO, P. A. BOREA, T. TUCCINARDI - 'Pharmacophore Based Receptor Modeling: The Case of Adenosine A3 Receptor Antagonists. An Approach to the Optimization of Protein Models.' (pubblicazione su rivista, 2006) JOURNAL OF MEDICINAL CHEMISTRY, Vol.49, 4085 - 4097

60) A. ANGELUCCI, S. SCHENONE, G. L. GRAVINA, P. MUZI, C. FESTUCCIA, C. VICENTINI, M. BOTTA, M. BOLOGNA - 'Pyrazolo [3,4-d] pyrimidines c-Src inhibitors reduce epidermal growth factor-induced migration in prostate cancer cells.' (pubblicazione su rivista, 2006) EUROPEAN JOURNAL OF CANCER, Vol.42, 2838 - 2845

61) F. CARRARO, A. NALDINI, A. PUCCI, G. A. LOCATELLI, G. MAGA, S. SCHENONE, O. BRUNO, A. RANISE, F. BONDAVALLI, C. BRULLO, P. FOSSA, G. MENOZZI, L. MOSTI, M. MODUGNO, C. TINTORI, F. MANETTI, M. BOTTA - 'Pyrazolo[3,4-d]pyrimidines as Potent Antiproliferative and Proapoptotic Agents toward A431 and 8701-BC Cells in Culture via Inhibition of c-Src Phosphorylation ' (pubblicazione su rivista, 2006) JOURNAL OF MEDICINAL CHEMISTRY, Vol.49, 1549 - 1561

62) T. SEMERARO, A. LOSSANI, M. BOTTA, C. GHIRON, R. ALVAREZ, F. MANETTI, C. MUGNAINI, S. VALENSIN, F. FOCHER, F. CORELLI - 'Simplified Analogues of Immucillin-G Retain Potent Human Purine Nucleoside Phosphorylase Inhibitory Activity' (pubblicazione su rivista, 2006) JOURNAL OF MEDICINAL CHEMISTRY, Vol.49, 6037 - 6045

63) A. TOGNINELLI, C. CARMI, E. PETRICCI, C. MUGNAINI, S. MASSA, F. CORELLI, M. BOTTA - 'Solution-phase parallel synthesis of S-DABO analogues' (pubblicazione su rivista, 2006) TETRAHEDRON LETTERS, Vol.47, 65 - 67

64) M. L. RENZULLI, L. ROCHEBLAVE, S. I. AVRAMOVA, E. GALLETTI, D. CASTAGNOLO, A. TAFI, F. CORELLI, M. BOTTA - 'Studies towards the synthesis of the bicyclic 3,8-secotaxane diterpenoid system using a ring closing metathesis strategy' (pubblicazione su rivista, 2006) TETRAHEDRON, Vol.63, 497 - 590

65) C. MUGNAINI, F. MANETTI, J. A. ESTÉ, I. CLOTET-CODINA, G. MAGA, R. CANCIO, M. BOTTA, F. CORELLI - 'Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors.' (pubblicazione su rivista, 2006) BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, Vol.16, 3541 – 3544

66) M. MAGNANI, F. ORTUSO, S. SORO, S. ALCARO, A. TRAMONTANO, M. BOTTA - 'The bI/bIII-tubulin isoforms and their complexes with antimitotic agents. Docking and molecular dynamics studies.' (pubblicazione su rivista, 2006) The FEBS Journal, Vol.273, 3301 - 3310

67) E. PETRICCI, C. MUGNAINI, M. RADI, A. TOGNINELLI, C. BERNARDINI, F. MANETTI, M. C. PARLATO, M. L. RENZULLI, M. ALONGI, C. FALCIANI, F. CORELLI, M. BOTTA - 'Towards new methodologies for the synthesis of biologically interesting 6-substituted pyrimidines and 4(3H)-pyrimidinones' (pubblicazione su rivista, 2006) ARKIVOC, Vol.vii, 452 - 478

68) A. PALADINO, C. MUGNAINI, M. BOTTA, F. CORELLI - 'A new linker for anchoring/masking primary amines on solid support' (pubblicazione su rivista, 2005) ORGANIC LETTERS, Vol.7, 565 - 568

69) A. TAFI, M. AGAMENNONE, P. TORTORELLA, S. ALCARO, C. GALLINA, M. BOTTA - 'AMBER force field implementation of the boronate function to simulate the inhibition of â-lactamases by alkyl and aryl boronic acids' (pubblicazione su rivista, 2005) EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, Vol.40, 1134 - 1142

70) R. DI SANTO, A. TAFI, R. COSTI, M. BOTTA, M. ARTICO, F. CORELLI, M. FORTE, F. CAPORUSCIO, L. ANGIOLELLA, A. PALAMARA - 'Antifungal Agents. 11.N-Substituted Derivatives of 1-[(Aryl)(4-aryl-1H-pyrrol-3yl)methyl]-1H-imidazole: Synthesis, Anti-Candida Activity, and QSAR Studies' (pubblicazione su rivista, 2005) J.MED.CHEM., Vol.48, 5140 - 5153

71) C. MUGNAINI, E. PETRICCI, F. CORELLI, M. BOTTA - 'Combinatorial chemistry as a tool for targeting different stages of the replicative HIV-1 cycle' (pubblicazione su rivista, 2005) COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING, Vol.8, 387 - 401

72) M. BIAVA, G. C. PORRETTA, A. CAPPELLI, S. VOMERO, F. MANETTI, M. BOTTA, L. SAUTEBIN, A. ROSSI, F. MAKOVEC, M. ANZINI - 'Diarylpyrrole-3-acetic Acids and Esters as Novel Classes of Potent and Selective COX-2 Inhibitors' (pubblicazione su rivista, 2005) Journal of Medicinal Chemistry, Vol.48, 3428 - 3432

73) M. ARMAND-UGON, I. CLOTET, C. TINTORI, F. MANETTI, B. CLOTET, M. BOTTA, J. A. ESTÉ - 'Homology modeling of HIV-1 gp120 and docking of molecules on its surface agree with experimental data' (pubblicazione su rivista, 2005) ANTIVIRAL RESEARCH, Vol.65, A29 - A29

74) D. CASTAGNOLO, M. L. RENZULLI, E. GALLETTI, F. CORELLI, M. BOTTA - 'Microwave-assisted ethylene-alkyne cross-metathesis: synthesis of chiral 2-(N-1-acetyl-1-arylmethyl)-1,3-butadienes' (pubblicazione su rivista, 2005) Tetrahedron: Asymmetry, Vol.16, 2893 - 2896

75) F. MANETTI, J. A. ESTE, I. CLOTET-CODINA, M. ARMAND-UGON, G. MAGA, E. CRESPAN, R. CANCIO, C. MUGNAINI, C. BERNARDINI, A. TOGNINELLI, C. CARMI, M. ALONGI, E. PETRICCI, S. MASSA, F. CORELLI, M. BOTTA - 'Parallel Solution-phase and Microwave-assisted Synthesis of New S-DABO Derivatives Endowed with Subnanomolar Anti-HIV-1 Activity' (pubblicazione su rivista, 2005) JOURNAL OF MEDICINAL CHEMISTRY, Vol.48, 8000 - 8008

76) F. MANETTI, S. SCHENONE, F. BONDAVALLI, C. BRULLO, O. BRUNO, A. RANISE, L. MOSTI, G. MENOZZI, P. FOSSA, M. . L. TRINCAVELLI, C. MARTINI, A. MARTINELLI, C. TINTORI, M. BOTTA - 'Synthesis and 3D QSAR of New Pyrazolo[3,4-b]pyridines: Potent and Selective Inhibitors of A1 Adenosine Receptors' (pubblicazione su rivista, 2005) JOURNAL OF MEDICINAL CHEMISTRY, Vol.48, 7172 - 7185

77) E. PATANÈ, V. PITTALÀ, F. GUERRERA, L. SALERNO, G. ROMEO, M. A. SIRACUSA, F. RUSSO, F. MANETTI, M. BOTTA, I. MEREGHETTI, A. CAGNOTTO, T. MENNINI - 'Synthesis of 3-Arylpiperazinylalkylpyrrolo[3,2-d]pyrimidine-2,4-dione Derivatives as Novel, Potent, and Selective alpha1-Adrenoceptor Ligands.' (pubblicazione su rivista, 2005) Journal Medicinal Chemistry, Vol.48, 2420 - 2431

78) M. RADI, C. MUGNAINI, E. PETRICCI, F. CORELLI, M. BOTTA - 'Synthesis of Reactive Cytidine Derivatives as Building Blocks for Cross-Linking Oligonucleotides' (pubblicazione su rivista, 2005) TETRAHEDRON LETTERS, Vol.46, 4361 - 4364

79) M. ARMAND-UGON, I. CLOTET-CODINA, C. TINTORI, F. MANETTI, B. CLOTET, M. BOTTA, J. A. ESTE - 'The anti-HIV activity of ADS-J1 targets the HIV-1 gp120' (pubblicazione su rivista, 2005) VIROLOGY, Vol.343, 141 - 149

80) M. RADI, E. PETRICCI, F. CORELLI, M. BOTTA – “Parallel solution phase synthesis of 4-dialkylamino-2-methylsulfonyl-6-vinylpyrimidines” (pubblicazione su rivista, 2005) JOURNAL OF COMBINATORIAL CHEMISTRY, Vol.7, 117 - 122

Patents
S. SCHENONE, F. BONDAVALLI, O. BRUNO, M. BOTTA, F. MANETTI, M. RADI, A. SANTUCCI, G. MAGA, M. BOLOGNA, A. ANGELUCCI, A. SANTUCCI, A. SPREAFICO, F. CARRARO - 'New 4-substituted derivatives of pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine and uses thereof ' (brevetto, 2008) M. BOTTA, M. RADI, F. MANETTI, G. BOTTA, G. MAGA, J. BORLAK - 'Derivati 1,3,4-tiadiazolici, metodi di preparazione e uso di essi. IT RM2007A000222' (brevetto, 2007)

M. BIAVA, F. MANETTI, R. POMPEI, A. DE LOGU, M. BOTTA, G. C. PORRETTA - 'Pyrrole compounds as inibitors of mycobacteria, synthesis thereof and intermediates thereto ' (brevetto, 2007)

M. BOTTA, F. MANETTI, R. POMPEI, M. BIAVA, D. DEIDDA, G. C. PORRETTA - 'Derivatives of 1-[1,5-bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl]methyl-4-methylpiperazine, synthesis process and uses thereof. WO2006092822.' (brevetto, 2006)

M. BIAVA, F. MANETTI, D. DEIDDA, R. POMPEI, M. BOTTA, G. C. PORRETTA - 'Derivati del 1-[1,5-di(4-clorofenil)-2-metil-1H-3-pirrolil]metil-4-metil piperazina (BM 212), procedimento per la loro produzione e uso di essi come antitubercolari. IT RM2005A000094.' (brevetto, 2005)

M. BOTTA, F. CORELLI, G. MAGA, E. PETRICCI, M. RADI - 'Derivati 6-vinil pirimidinici e pirimidinonici, e loro usi' (brevetto, 2005)

F. BONDAVALLI, M. BOTTA, S. DONNINI, F. MANETTI, S. SCHENONE, M. ZICHE - '4-Substituted derivatives of pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine and uses thereof. WO2004106339' (brevetto, 2004)

F. BONDAVALLI, M. BOTTA, O. BRUNO, F. CARRARO, F. MANETTI, S. SCHENONE - '4-Substituted derivatives of pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine and uses thereof. WO2004106340.' (brevetto, 2004)

F. BONDAVALLI, M. BOTTA, O. BRUNO, F. MANETTI, S. SCHENONE - 'Derivati 4-sostituiti della 1-(2-cloro-2-feniletil)-1H-pirazolo[3,4-d]pirimidina e loro usi. IT RM2003000263.' (brevetto, 2003)

F. BONDAVALLI, M. BOTTA, S. DONNINI, F. MANETTI, S. SCHENONE, M. ZICHE - 'Derivati 4-sostituiti della 1-(2-cloro-2-feniletil)-1H-pirazolo[3,4-d]pirimidina e loro usi. IT RM2003A000264.' (brevetto, 2003)

M. BOTTA, C. CRESCENZI, D. MANCINETTI, M. POMPEI, F. BONIFACIO – ‘Diastereoselective process for the preparation of the antiviral agent 4-amino-1-(2R-Hydroxymethyl-[1,3]Oxathiolan-5S-YL)-1H-Pyrimidin-2-One’. WO03/040139 (brevetto 2003)

L. BETTI, M. BOTTA, M. FLORIDI, G. GIANNACCINI, F. MANETTI, G. STRAPPAGHETTI - 'Composti Derivati del Piridazinone Antagonisti dei Recettori a1 Adrenergici, loro Impiego in Campo Medico e Procedimento di Preparazione. IT RM2002A000362' (brevetto, 2002)

GIANNESSI, F., TASSONI, E., TINTI, M. O., PESSOTTO, P., BOTTA, M., CORELLI, F. ‘Derivati di Guanidine Variamente Sostituite, loro Uso Come Medicamenti ad Attività Antidiabetica e/o Antiobesità’. RM2002A000625 (brevetto 2002)

BOTTA, M., CRESCENZI, C., POMPEI, M., BONIFACIO, F., MANCINETTI, D. ‘Processo Diastereoselettivo per la Preparazione dell'Agente Antivirale 4-amino-1-(2R-idrossimetil-[1,3]ossatiolan-5S-IL)-1H-pirimidin-2-one’. MI2001A002317 (brevetto 2001)

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