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1.
Biochemical and transcriptional profiling to triage additional activities in a series of IGF-1R/IR inhibitors.
Bioorg Med Chem;
20(6): 1961-72, 2012 Mar 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-22137930
2.
Proline isosteres in a series of 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitors of IGF-1R kinase and IR kinase.
Bioorg Med Chem Lett;
20(17): 5027-30, 2010 Sep 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-20675137
3.
Insulin-like growth factor-1 receptor (IGF-1R) kinase inhibitors: SAR of a series of 3-[6-(4-substituted-piperazin-1-yl)-4-methyl-1H-benzimidazol-2-yl]-1H-pyridine-2-one.
Bioorg Med Chem Lett;
20(10): 3182-5, 2010 May 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-20399649
4.
SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors.
Bioorg Med Chem Lett;
20(5): 1744-8, 2010 Mar 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-20153189
5.
2-(1H-Imidazol-4-yl)ethanamine and 2-(1H-pyrazol-1-yl)ethanamine side chain variants of the IGF-1R inhibitor BMS-536924.
Bioorg Med Chem Lett;
18(5): 1702-7, 2008 Mar 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-18258427
6.
Balancing oral exposure with Cyp3A4 inhibition in benzimidazole-based IGF-IR inhibitors.
Bioorg Med Chem Lett;
18(14): 4075-80, 2008 Jul 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-18572407
7.
Discovery of a fluoroindolo[2,3-a]carbazole clinical candidate with broad spectrum antitumor activity in preclinical tumor models superior to the marketed oncology drug, CPT-11.
J Med Chem;
48(7): 2258-61, 2005 Apr 07.
Artículo
en Inglés
| MEDLINE | ID: mdl-15801816
8.
Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity.
J Med Chem;
48(18): 5639-43, 2005 Sep 08.
Artículo
en Inglés
| MEDLINE | ID: mdl-16134929
9.
Novel 3',6'-anhydro and N12,N13-bridged glycosylated fluoroindolo[2,3-a]carbazoles as topoisomerase I inhibitors. Fluorine as a leaving group from sp3 carbon.
Org Lett;
7(7): 1271-4, 2005 Mar 31.
Artículo
en Inglés
| MEDLINE | ID: mdl-15787484
10.
Discovery of antitumor indolocarbazoles: rebeccamycin, NSC 655649, and fluoroindolocarbazoles.
Curr Med Chem Anticancer Agents;
2(2): 255-66, 2002 Mar.
Artículo
en Inglés
| MEDLINE | ID: mdl-12678746
11.
Design and synthesis of a fluoroindolocarbazole series as selective topoisomerase I active agents. Discovery of water-soluble 3,9-difluoro-12,13-dihydro-13-[6-amino-beta-D-glucopyranosyl]-5H,13H-benzo[b]- thienyl[2,3-a]pyrrolo[3,4-c]carbazole- 5,7(6H)-dione (BMS-251873) with curative antitumor activity against prostate carcinoma xenograft tumor model.
J Med Chem;
47(7): 1609-12, 2004 Mar 25.
Artículo
en Inglés
| MEDLINE | ID: mdl-15027851
12.
Nucleophilic capture of the imino-quinone methide type intermediates generated from 2-aminothiazol-5-yl carbinols.
Org Lett;
11(22): 5154-7, 2009 Nov 19.
Artículo
en Inglés
| MEDLINE | ID: mdl-19827772
13.
BMS-754807, a small molecule inhibitor of insulin-like growth factor-1R/IR.
Mol Cancer Ther;
8(12): 3341-9, 2009 Dec.
Artículo
en Inglés
| MEDLINE | ID: mdl-19996272
14.
Discovery of a 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in clinical development.
J Med Chem;
52(23): 7360-3, 2009 Dec 10.
Artículo
en Inglés
| MEDLINE | ID: mdl-19778024
15.
Discovery and preclinical evaluation of [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic acid, (3S)-3-morpholinylmethyl ester (BMS-599626), a selective and orally efficacious inhibitor of human epidermal growth factor receptor 1 and 2 kinases.
J Med Chem;
52(21): 6527-30, 2009 Nov 12.
Artículo
en Inglés
| MEDLINE | ID: mdl-19821562
16.
Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinase with broad spectrum in vivo antitumor activity.
J Med Chem;
51(19): 5897-900, 2008 Oct 09.
Artículo
en Inglés
| MEDLINE | ID: mdl-18763755
17.
Imidazole moiety replacements in the 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one inhibitors of insulin-like growth factor receptor-1 (IGF-1R) to improve cytochrome P450 profile.
Bioorg Med Chem Lett;
17(11): 3072-6, 2007 Jun 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-17398093
18.
Synthesis and structure-activity relationship of imidazo(1,2-a)thieno(3,2-e)pyrazines as IKK-beta inhibitors.
Bioorg Med Chem Lett;
17(15): 4284-9, 2007 Aug 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-17540562
19.
Synthesis and biological evaluation of 4-amino derivatives of benzimidazoquinoxaline, benzimidazoquinoline, and benzopyrazoloquinazoline as potent IKK inhibitors.
Bioorg Med Chem Lett;
17(5): 1233-7, 2007 Mar 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-17197177
20.
Discovery and initial SAR of 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-ones as inhibitors of insulin-like growth factor 1-receptor (IGF-1R).
Bioorg Med Chem Lett;
17(8): 2317-21, 2007 Apr 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-17317169