Li A - Search Results

1

BMS-754807, a small molecule inhibitor of insulin-like growth factor-1R/IR.

Carboni JM, Wittman M, Yang Z, Lee F, Greer A, Hurlburt W, Hillerman S, Cao C, Cantor GH, Dell-John J, Chen C, Discenza L, Menard K, Li A, Trainor G, Vyas D, Kramer R, Attar RM, Gottardis MM. Carboni JM, et al. Among authors: li a. Mol Cancer Ther. 2009 Dec;8(12):3341-9. doi: 10.1158/1535-7163.MCT-09-0499. Mol Cancer Ther. 2009. PMID: 19996272

2

Tumor development by transgenic expression of a constitutively active insulin-like growth factor I receptor.

Carboni JM, Lee AV, Hadsell DL, Rowley BR, Lee FY, Bol DK, Camuso AE, Gottardis M, Greer AF, Ho CP, Hurlburt W, Li A, Saulnier M, Velaparthi U, Wang C, Wen ML, Westhouse RA, Wittman M, Zimmermann K, Rupnow BA, Wong TW. Carboni JM, et al. Among authors: li a. Cancer Res. 2005 May 1;65(9):3781-7. doi: 10.1158/0008-5472.CAN-04-4602. Cancer Res. 2005. PMID: 15867374

3

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.

Wittman M, Carboni J, Attar R, Balasubramanian B, Balimane P, Brassil P, Beaulieu F, Chang C, Clarke W, Dell J, Eummer J, Frennesson D, Gottardis M, Greer A, Hansel S, Hurlburt W, Jacobson B, Krishnananthan S, Lee FY, Li A, Lin TA, Liu P, Ouellet C, Sang X, Saulnier MG, Stoffan K, Sun Y, Velaparthi U, Wong H, Yang Z, Zimmermann K, Zoeckler M, Vyas D. Wittman M, et al. Among authors: li a. J Med Chem. 2005 Sep 8;48(18):5639-43. doi: 10.1021/jm050392q. J Med Chem. 2005. PMID: 16134929

4

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).

Velaparthi U, Wittman M, Liu P, Stoffan K, Zimmermann K, Sang X, Carboni J, Li A, Attar R, Gottardis M, Greer A, Chang CY, Jacobsen BL, Sack JS, Sun Y, Langley DR, Balasubramanian B, Vyas D. Velaparthi U, et al. Among authors: li a. Bioorg Med Chem Lett. 2007 Apr 15;17(8):2317-21. doi: 10.1016/j.bmcl.2007.01.102. Epub 2007 Feb 4. Bioorg Med Chem Lett. 2007. PMID: 17317169

5

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.

Velaparthi U, Liu P, Balasubramanian B, Carboni J, Attar R, Gottardis M, Li A, Greer A, Zoeckler M, Wittman MD, Vyas D. Velaparthi U, et al. Among authors: li a. Bioorg Med Chem Lett. 2007 Jun 1;17(11):3072-6. doi: 10.1016/j.bmcl.2007.03.048. Epub 2007 Mar 19. Bioorg Med Chem Lett. 2007. PMID: 17398093

6

2-(1H-Imidazol-4-yl)ethanamine and 2-(1H-pyrazol-1-yl)ethanamine side chain variants of the IGF-1R inhibitor BMS-536924.

Saulnier MG, Frennesson DB, Wittman MD, Zimmermann K, Velaparthi U, Langley DR, Struzynski C, Sang X, Carboni J, Li A, Greer A, Yang Z, Balimane P, Gottardis M, Attar R, Vyas D. Saulnier MG, et al. Among authors: li a. Bioorg Med Chem Lett. 2008 Mar 1;18(5):1702-7. doi: 10.1016/j.bmcl.2008.01.049. Epub 2008 Jan 18. Bioorg Med Chem Lett. 2008. PMID: 18258427

7

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.

Velaparthi U, Wittman M, Liu P, Carboni JM, Lee FY, Attar R, Balimane P, Clarke W, Sinz MW, Hurlburt W, Patel K, Discenza L, Kim S, Gottardis M, Greer A, Li A, Saulnier M, Yang Z, Zimmermann K, Trainor G, Vyas D. Velaparthi U, et al. Among authors: li a. J Med Chem. 2008 Oct 9;51(19):5897-900. doi: 10.1021/jm800832q. Epub 2008 Sep 3. J Med Chem. 2008. PMID: 18763755

8

The mechanisms of differential sensitivity to an insulin-like growth factor-1 receptor inhibitor (BMS-536924) and rationale for combining with EGFR/HER2 inhibitors.

Huang F, Greer A, Hurlburt W, Han X, Hafezi R, Wittenberg GM, Reeves K, Chen J, Robinson D, Li A, Lee FY, Gottardis MM, Clark E, Helman L, Attar RM, Dongre A, Carboni JM. Huang F, et al. Among authors: li a. Cancer Res. 2009 Jan 1;69(1):161-70. doi: 10.1158/0008-5472.CAN-08-0835. Cancer Res. 2009. PMID: 19117999 Free PMC article.

9

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.

Wittman MD, Carboni JM, Yang Z, Lee FY, Antman M, Attar R, Balimane P, Chang C, Chen C, Discenza L, Frennesson D, Gottardis MM, Greer A, Hurlburt W, Johnson W, Langley DR, Li A, Li J, Liu P, Mastalerz H, Mathur A, Menard K, Patel K, Sack J, Sang X, Saulnier M, Smith D, Stefanski K, Trainor G, Velaparthi U, Zhang G, Zimmermann K, Vyas DM. Wittman MD, et al. Among authors: li j, li a. J Med Chem. 2009 Dec 10;52(23):7360-3. doi: 10.1021/jm900786r. J Med Chem. 2009. PMID: 19778024

10

SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors.

Zimmermann K, Wittman MD, Saulnier MG, Velaparthi U, Sang X, Frennesson DB, Struzynski C, Seitz SP, He L, Carboni JM, Li A, Greer AF, Gottardis M, Attar RM, Yang Z, Balimane P, Discenza LN, Lee FY, Sinz M, Kim S, Vyas D. Zimmermann K, et al. Among authors: li a. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1744-8. doi: 10.1016/j.bmcl.2010.01.087. Epub 2010 Jan 21. Bioorg Med Chem Lett. 2010. PMID: 20153189

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