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Items: 28

1.

Novel pyrrole carboxamide inhibitors of JAK2 as potential treatment of myeloproliferative disorders.

Brasca MG, Gnocchi P, Nesi M, Amboldi N, Avanzi N, Bertrand J, Bindi S, Canevari G, Casero D, Ciomei M, Colombo N, Cribioli S, Fachin G, Felder ER, Galvani A, Isacchi A, Motto I, Panzeri A, Donati D.

Bioorg Med Chem. 2015 May 15;23(10):2387-407. doi: 10.1016/j.bmc.2015.03.059. Epub 2015 Mar 28.

PMID:
25882525
2.

Pyrrole-3-carboxamides as potent and selective JAK2 inhibitors.

Brasca MG, Nesi M, Avanzi N, Ballinari D, Bandiera T, Bertrand J, Bindi S, Canevari G, Carenzi D, Casero D, Ceriani L, Ciomei M, Cirla A, Colombo M, Cribioli S, Cristiani C, Della Vedova F, Fachin G, Fasolini M, Felder ER, Galvani A, Isacchi A, Mirizzi D, Motto I, Panzeri A, Pesenti E, Vianello P, Gnocchi P, Donati D.

Bioorg Med Chem. 2014 Sep 1;22(17):4998-5012. doi: 10.1016/j.bmc.2014.06.025. Epub 2014 Jun 21.

PMID:
25009002
3.

Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.

Casale E, Amboldi N, Brasca MG, Caronni D, Colombo N, Dalvit C, Felder ER, Fogliatto G, Galvani A, Isacchi A, Polucci P, Riceputi L, Sola F, Visco C, Zuccotto F, Casuscelli F.

Bioorg Med Chem. 2014 Aug 1;22(15):4135-50. doi: 10.1016/j.bmc.2014.05.056. Epub 2014 Jun 14.

PMID:
24980703
4.

Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).

Brasca MG, Mantegani S, Amboldi N, Bindi S, Caronni D, Casale E, Ceccarelli W, Colombo N, De Ponti A, Donati D, Ermoli A, Fachin G, Felder ER, Ferguson RD, Fiorelli C, Guanci M, Isacchi A, Pesenti E, Polucci P, Riceputi L, Sola F, Visco C, Zuccotto F, Fogliatto G.

Bioorg Med Chem. 2013 Nov 15;21(22):7047-63. doi: 10.1016/j.bmc.2013.09.018. Epub 2013 Sep 19. Erratum in: Bioorg Med Chem. 2014 Jan 1;22(1):662.

PMID:
24100158
5.

NMS-E973, a novel synthetic inhibitor of Hsp90 with activity against multiple models of drug resistance to targeted agents, including intracranial metastases.

Fogliatto G, Gianellini L, Brasca MG, Casale E, Ballinari D, Ciomei M, Degrassi A, De Ponti A, Germani M, Guanci M, Paolucci M, Polucci P, Russo M, Sola F, Valsasina B, Visco C, Zuccotto F, Donati D, Felder E, Pesenti E, Galvani A, Mantegani S, Isacchi A.

Clin Cancer Res. 2013 Jul 1;19(13):3520-32. doi: 10.1158/1078-0432.CCR-12-3512. Epub 2013 May 14.

6.

Anti-tumour efficacy on glioma models of PHA-848125, a multi-kinase inhibitor able to cross the blood-brain barrier.

Albanese C, Alzani R, Amboldi N, Degrassi A, Festuccia C, Fiorentini F, Gravina G, Mercurio C, Pastori W, Brasca M, Pesenti E, Galvani A, Ciomei M.

Br J Pharmacol. 2013 May;169(1):156-66. doi: 10.1111/bph.12112.

7.

Down-regulation of the PTTG1 proto-oncogene contributes to the melanoma suppressive effects of the cyclin-dependent kinase inhibitor PHA-848125.

Caporali S, Alvino E, Levati L, Esposito AI, Ciomei M, Brasca MG, Del Bufalo D, Desideri M, Bonmassar E, Pfeffer U, D'Atri S.

Biochem Pharmacol. 2012 Sep 1;84(5):598-611. doi: 10.1016/j.bcp.2012.06.004. Epub 2012 Jun 13.

PMID:
22704958
8.

5-(2-amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one derivatives as new classes of selective and orally available Polo-like kinase 1 inhibitors.

Caruso M, Valsasina B, Ballinari D, Bertrand J, Brasca MG, Caldarelli M, Cappella P, Fiorentini F, Gianellini LM, Scolaro A, Beria I.

Bioorg Med Chem Lett. 2012 Jan 1;22(1):96-101. doi: 10.1016/j.bmcl.2011.11.065. Epub 2011 Nov 23.

PMID:
22154349
9.

NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor.

Beria I, Bossi RT, Brasca MG, Caruso M, Ceccarelli W, Fachin G, Fasolini M, Forte B, Fiorentini F, Pesenti E, Pezzetta D, Posteri H, Scolaro A, Re Depaolini S, Valsasina B.

Bioorg Med Chem Lett. 2011 May 15;21(10):2969-74. doi: 10.1016/j.bmcl.2011.03.054. Epub 2011 Mar 21.

PMID:
21470862
10.

4,5-Dihydro-1H-pyrazolo[4,3-h]quinazolines as potent and selective Polo-like kinase 1 (PLK1) inhibitors.

Beria I, Valsasina B, Brasca MG, Ceccarelli W, Colombo M, Cribioli S, Fachin G, Ferguson RD, Fiorentini F, Gianellini LM, Giorgini ML, Moll JK, Posteri H, Pezzetta D, Roletto F, Sola F, Tesei D, Caruso M.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6489-94. doi: 10.1016/j.bmcl.2010.09.060. Epub 2010 Sep 17.

PMID:
20932759
11.

Dual targeting of CDK and tropomyosin receptor kinase families by the oral inhibitor PHA-848125, an agent with broad-spectrum antitumor efficacy.

Albanese C, Alzani R, Amboldi N, Avanzi N, Ballinari D, Brasca MG, Festuccia C, Fiorentini F, Locatelli G, Pastori W, Patton V, Roletto F, Colotta F, Galvani A, Isacchi A, Moll J, Pesenti E, Mercurio C, Ciomei M.

Mol Cancer Ther. 2010 Aug;9(8):2243-54. doi: 10.1158/1535-7163.MCT-10-0190. Epub 2010 Aug 3.

12.

Transcriptional analysis of an E2F gene signature as a biomarker of activity of the cyclin-dependent kinase inhibitor PHA-793887 in tumor and skin biopsies from a phase I clinical study.

Locatelli G, Bosotti R, Ciomei M, Brasca MG, Calogero R, Mercurio C, Fiorentini F, Bertolotti M, Scacheri E, Scaburri A, Galvani A, Pesenti E, De Baere T, Soria JC, Lazar V, Isacchi A.

Mol Cancer Ther. 2010 May;9(5):1265-73. doi: 10.1158/1535-7163.MCT-09-1163. Epub 2010 Apr 27.

13.

Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors.

Beria I, Ballinari D, Bertrand JA, Borghi D, Bossi RT, Brasca MG, Cappella P, Caruso M, Ceccarelli W, Ciavolella A, Cristiani C, Croci V, De Ponti A, Fachin G, Ferguson RD, Lansen J, Moll JK, Pesenti E, Posteri H, Perego R, Rocchetti M, Storici P, Volpi D, Valsasina B.

J Med Chem. 2010 May 13;53(9):3532-51. doi: 10.1021/jm901713n.

PMID:
20397705
14.

Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.

Brasca MG, Albanese C, Alzani R, Amici R, Avanzi N, Ballinari D, Bischoff J, Borghi D, Casale E, Croci V, Fiorentini F, Isacchi A, Mercurio C, Nesi M, Orsini P, Pastori W, Pesenti E, Pevarello P, Roussel P, Varasi M, Volpi D, Vulpetti A, Ciomei M.

Bioorg Med Chem. 2010 Mar 1;18(5):1844-53. doi: 10.1016/j.bmc.2010.01.042. Epub 2010 Jan 25.

PMID:
20153204
15.

Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.

Traquandi G, Ciomei M, Ballinari D, Casale E, Colombo N, Croci V, Fiorentini F, Isacchi A, Longo A, Mercurio C, Panzeri A, Pastori W, Pevarello P, Volpi D, Roussel P, Vulpetti A, Brasca MG.

J Med Chem. 2010 Mar 11;53(5):2171-87. doi: 10.1021/jm901710h.

PMID:
20141146
16.

The cyclin-dependent kinase inhibitor PHA-848125 suppresses the in vitro growth of human melanomas sensitive or resistant to temozolomide, and shows synergistic effects in combination with this triazene compound.

Caporali S, Alvino E, Starace G, Ciomei M, Brasca MG, Levati L, Garbin A, Castiglia D, Covaciu C, Bonmassar E, D'Atri S.

Pharmacol Res. 2010 May;61(5):437-48. doi: 10.1016/j.phrs.2009.12.009. Epub 2009 Dec 21.

PMID:
20026273
17.

Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor.

Brasca MG, Amboldi N, Ballinari D, Cameron A, Casale E, Cervi G, Colombo M, Colotta F, Croci V, D'Alessio R, Fiorentini F, Isacchi A, Mercurio C, Moretti W, Panzeri A, Pastori W, Pevarello P, Quartieri F, Roletto F, Traquandi G, Vianello P, Vulpetti A, Ciomei M.

J Med Chem. 2009 Aug 27;52(16):5152-63. doi: 10.1021/jm9006559.

PMID:
19603809
18.

Cell division cycle 7 kinase inhibitors: 1H-pyrrolo[2,3-b]pyridines, synthesis and structure-activity relationships.

Ermoli A, Bargiotti A, Brasca MG, Ciavolella A, Colombo N, Fachin G, Isacchi A, Menichincheri M, Molinari A, Montagnoli A, Pillan A, Rainoldi S, Sirtori FR, Sola F, Thieffine S, Tibolla M, Valsasina B, Volpi D, Santocanale C, Vanotti E.

J Med Chem. 2009 Jul 23;52(14):4380-90. doi: 10.1021/jm900248g.

PMID:
19555113
19.

The synthesis of azadirachtin: a potent insect antifeedant.

Ley SV, Abad-Somovilla A, Anderson JC, Ayats C, Bänteli R, Beckmann E, Boyer A, Brasca MG, Brice A, Broughton HB, Burke BJ, Cleator E, Craig D, Denholm AA, Denton RM, Durand-Reville T, Gobbi LB, Göbel M, Gray BL, Grossmann RB, Gutteridge CE, Hahn N, Harding SL, Jennens DC, Jennens L, Lovell PJ, Lovell HJ, de la Puente ML, Kolb HC, Koot WJ, Maslen SL, McCusker CF, Mattes A, Pape AR, Pinto A, Santafianos D, Scott JS, Smith SC, Somers AQ, Spilling CD, Stelzer F, Toogood PL, Turner RM, Veitch GE, Wood A, Zumbrunn C.

Chemistry. 2008;14(34):10683-704. doi: 10.1002/chem.200801103.

PMID:
18821532
20.

6-Substituted pyrrolo[3,4-c]pyrazoles: an improved class of CDK2 inhibitors.

Brasca MG, Albanese C, Amici R, Ballinari D, Corti L, Croci V, Fancelli D, Fiorentini F, Nesi M, Orsini P, Orzi F, Pastori W, Perrone E, Pesenti E, Pevarello P, Riccardi-Sirtori F, Roletto F, Roussel P, Varasi M, Vulpetti A, Mercurio C.

ChemMedChem. 2007 Jun;2(6):841-52.

PMID:
17450625
21.

Polyfluorinated amino acids for sensitive 19F NMR-based screening and kinetic measurements.

Papeo G, Giordano P, Brasca MG, Buzzo F, Caronni D, Ciprandi F, Mongelli N, Veronesi M, Vulpetti A, Dalvit C.

J Am Chem Soc. 2007 May 2;129(17):5665-72. Epub 2007 Apr 7.

PMID:
17417847
22.

A practical synthesis of the major 3-hydroxy-2-pyrrolidinone metabolite of a potent CDK2/cyclin A inhibitor.

Nesi M, Borghi D, Brasca MG, Fiorentini F, Pevarello P.

Bioorg Med Chem Lett. 2006 Jun 15;16(12):3205-8. Epub 2006 Apr 17.

PMID:
16616492
23.

3-Amino-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: a new class of CDK2 inhibitors.

Pevarello P, Fancelli D, Vulpetti A, Amici R, Villa M, Pittalà V, Vianello P, Cameron A, Ciomei M, Mercurio C, Bischoff JR, Roletto F, Varasi M, Brasca MG.

Bioorg Med Chem Lett. 2006 Feb 15;16(4):1084-90. Epub 2005 Nov 14.

PMID:
16290148
24.

Structure-based approaches to improve selectivity: CDK2-GSK3beta binding site analysis.

Vulpetti A, Crivori P, Cameron A, Bertrand J, Brasca MG, D'Alessio R, Pevarello P.

J Chem Inf Model. 2005 Sep-Oct;45(5):1282-90.

PMID:
16180905
25.

3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 2. Lead optimization.

Pevarello P, Brasca MG, Orsini P, Traquandi G, Longo A, Nesi M, Orzi F, Piutti C, Sansonna P, Varasi M, Cameron A, Vulpetti A, Roletto F, Alzani R, Ciomei M, Albanese C, Pastori W, Marsiglio A, Pesenti E, Fiorentini F, Bischoff JR, Mercurio C.

J Med Chem. 2005 Apr 21;48(8):2944-56. Erratum in: J Med Chem. 2005 Jul 28;48(15):5058.

PMID:
15828833
26.

Benzodipyrazoles: a new class of potent CDK2 inhibitors.

D'Alessio R, Bargiotti A, Metz S, Brasca MG, Cameron A, Ermoli A, Marsiglio A, Polucci P, Roletto F, Tibolla M, Vazquez ML, Vulpetti A, Pevarello P.

Bioorg Med Chem Lett. 2005 Mar 1;15(5):1315-9.

PMID:
15713378
27.

3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding.

Pevarello P, Brasca MG, Amici R, Orsini P, Traquandi G, Corti L, Piutti C, Sansonna P, Villa M, Pierce BS, Pulici M, Giordano P, Martina K, Fritzen EL, Nugent RA, Casale E, Cameron A, Ciomei M, Roletto F, Isacchi A, Fogliatto G, Pesenti E, Pastori W, Marsiglio A, Leach KL, Clare PM, Fiorentini F, Varasi M, Vulpetti A, Warpehoski MA.

J Med Chem. 2004 Jun 17;47(13):3367-80.

PMID:
15189033
28.

Cinnamamide analogs as inhibitors of protein tyrosine kinases.

Buzzetti F, Brasca MG, Crugnola A, Fustinoni S, Longo A, Penco S, Dalla Zonca P, Comoglio PM.

Farmaco. 1993 May;48(5):615-36.

PMID:
8343210

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