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Items: 1 to 20 of 80

1.

Balancing oral exposure with Cyp3A4 inhibition in benzimidazole-based IGF-IR inhibitors.

Zimmermann K, Wittman MD, Saulnier MG, Velaparthi U, Langley DR, Sang X, Frennesson D, Carboni J, Li A, Greer A, Gottardis M, Attar RM, Yang Z, Balimane P, Discenza LN, Vyas D.

Bioorg Med Chem Lett. 2008 Jul 15;18(14):4075-80. doi: 10.1016/j.bmcl.2008.05.104. Epub 2008 Jun 21.

PMID:
18572407
2.

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.

Velaparthi U, Saulnier MG, Wittman MD, Liu P, Frennesson DB, Zimmermann K, Carboni JM, Gottardis M, Li A, Greer A, Clarke W, Yang Z, Menard K, Lee FY, Trainor G, Vyas D.

Bioorg Med Chem Lett. 2010 May 15;20(10):3182-5. doi: 10.1016/j.bmcl.2010.03.057. Epub 2010 Mar 27.

PMID:
20399649
3.

Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R).

Emmitte KA, Wilson BJ, Baum EW, Emerson HK, Kuntz KW, Nailor KE, Salovich JM, Smith SC, Cheung M, Gerding RM, Stevens KL, Uehling DE, Mook RA Jr, Moorthy GS, Dickerson SH, Hassell AM, Leesnitzer MA, Shewchuk LM, Groy A, Rowand JL, Anderson K, Atkins CL, Yang J, Sabbatini P, Kumar R.

Bioorg Med Chem Lett. 2009 Feb 1;19(3):1004-8. doi: 10.1016/j.bmcl.2008.11.058. Epub 2008 Nov 20.

PMID:
19101143
4.

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.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1744-8. doi: 10.1016/j.bmcl.2010.01.087. Epub 2010 Jan 21.

PMID:
20153189
5.

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.

J Med Chem. 2008 Oct 9;51(19):5897-900. doi: 10.1021/jm800832q. Epub 2008 Sep 3.

PMID:
18763755
6.

Benzimidazole- and benzoxazole-based inhibitors of Rho kinase.

Sessions EH, Yin Y, Bannister TD, Weiser A, Griffin E, Pocas J, Cameron MD, Ruiz C, Lin L, Schürer SC, Schröter T, LoGrasso P, Feng Y.

Bioorg Med Chem Lett. 2008 Dec 15;18(24):6390-3. doi: 10.1016/j.bmcl.2008.10.095. Epub 2008 Oct 25.

PMID:
18996009
7.

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.

Cancer Res. 2009 Jan 1;69(1):161-70. doi: 10.1158/0008-5472.CAN-08-0835.

8.

Zwitterionic uracil derivatives as potent GnRH receptor antagonists with improved pharmaceutical properties.

Regan CF, Guo Z, Chen Y, Huang CQ, Chen M, Jiang W, Rueter JK, Coon T, Chen C, Saunders J, Brown MS, Betz SF, Struthers RS, Yang C, Wen J, Madan A, Zhu YF.

Bioorg Med Chem Lett. 2008 Aug 15;18(16):4503-7. doi: 10.1016/j.bmcl.2008.07.059. Epub 2008 Jul 17.

PMID:
18667310
9.

1,3-Disubstituted-imidazo[1,5-a]pyrazines as insulin-like growth-factor-I receptor (IGF-IR) inhibitors.

Mulvihill MJ, Ji QS, Werner D, Beck P, Cesario C, Cooke A, Cox M, Crew A, Dong H, Feng L, Foreman KW, Mak G, Nigro A, O'Connor M, Saroglou L, Stolz KM, Sujka I, Volk B, Weng Q, Wilkes R.

Bioorg Med Chem Lett. 2007 Feb 15;17(4):1091-7. Epub 2006 Nov 10.

PMID:
17127062
10.

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.

Bioorg Med Chem Lett. 2007 Apr 15;17(8):2317-21. Epub 2007 Feb 4.

PMID:
17317169
11.

Itk kinase inhibitors: initial efforts to improve the metabolical stability and the cell activity of the benzimidazole lead.

Moriarty KJ, Winters M, Qiao L, Ryan D, DesJarlis R, Robinson D, Cook BN, Kashem MA, Kaplita PV, Liu LH, Farrell TM, Khine HH, King J, Pullen SS, Roth GP, Magolda R, Takahashi H.

Bioorg Med Chem Lett. 2008 Oct 15;18(20):5537-40. doi: 10.1016/j.bmcl.2008.09.017. Epub 2008 Sep 7.

PMID:
18819794
12.

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.

Bioorg Med Chem Lett. 2007 Jun 1;17(11):3072-6. Epub 2007 Mar 19.

PMID:
17398093
13.

Insulin-like growth factor-I receptor blockade reduces the invasiveness of gastrointestinal cancers via blocking production of matrilysin.

Adachi Y, Li R, Yamamoto H, Min Y, Piao W, Wang Y, Imsumran A, Li H, Arimura Y, Lee CT, Imai K, Carbone DP, Shinomura Y.

Carcinogenesis. 2009 Aug;30(8):1305-13. doi: 10.1093/carcin/bgp134. Epub 2009 Jun 3.

PMID:
19493905
14.

Novel 1H-(benzimidazol-2-yl)-1H-pyridin-2-one inhibitors of insulin-like growth factor I (IGF-1R) kinase.

Wittman MD, Balasubramanian B, Stoffan K, Velaparthi U, Liu P, Krishnanathan S, Carboni J, Li A, Greer A, Attar R, Gottardis M, Chang C, Jacobson B, Sun Y, Hansel S, Zoeckler M, Vyas DM.

Bioorg Med Chem Lett. 2007 Feb 15;17(4):974-7. Epub 2006 Nov 17.

PMID:
17187980
15.

Phosphorylated insulin-like growth factor-i/insulin receptor is present in all breast cancer subtypes and is related to poor survival.

Law JH, Habibi G, Hu K, Masoudi H, Wang MY, Stratford AL, Park E, Gee JM, Finlay P, Jones HE, Nicholson RI, Carboni J, Gottardis M, Pollak M, Dunn SE.

Cancer Res. 2008 Dec 15;68(24):10238-46. doi: 10.1158/0008-5472.CAN-08-2755.

16.

5-Aminomethyl-1H-benzimidazoles as orally active inhibitors of inducible T-cell kinase (Itk).

Winters MP, Robinson DJ, Khine HH, Pullen SS, Woska JR Jr, Raymond EL, Sellati R, Cywin CL, Snow RJ, Kashem MA, Wolak JP, King J, Kaplita PV, Liu LH, Farrell TM, DesJarlais R, Roth GP, Takahashi H, Moriarty KJ.

Bioorg Med Chem Lett. 2008 Oct 15;18(20):5541-4. doi: 10.1016/j.bmcl.2008.09.016. Epub 2008 Sep 7.

PMID:
18823779
17.

Prediction of the effect of erythromycin, diltiazem, and their metabolites, alone and in combination, on CYP3A4 inhibition.

Zhang X, Jones DR, Hall SD.

Drug Metab Dispos. 2009 Jan;37(1):150-60. doi: 10.1124/dmd.108.022178. Epub 2008 Oct 14.

18.

Discovery of an inhibitor of insulin-like growth factor 1 receptor activation: implications for cellular potency and selectivity over insulin receptor.

Wood ER, Shewchuk L, Hassel A, Nichols J, Truesdale AT, Smith D, Carter HL, Weaver K, Barrett G, Leesnitzer T, Alvarez E, Bardera AI, Alamillo A, Cantizani J, Martin J, Smith GK, Jensen DE, Xie H, Mook R, Kumar R, Kuntz K.

Biochem Pharmacol. 2009 Dec 15;78(12):1438-47. doi: 10.1016/j.bcp.2009.07.022. Epub 2009 Aug 7.

PMID:
19665448
19.

Respiratory syncytial virus fusion inhibitors. Part 6: an examination of the effect of structural variation of the benzimidazol-2-one heterocycle moiety.

Combrink KD, Gulgeze HB, Thuring JW, Yu KL, Civiello RL, Zhang Y, Pearce BC, Yin Z, Langley DR, Kadow KF, Cianci CW, Li Z, Clarke J, Genovesi EV, Medina I, Lamb L, Yang Z, Zadjura L, Krystal M, Meanwell NA.

Bioorg Med Chem Lett. 2007 Sep 1;17(17):4784-90. Epub 2007 Jun 26.

PMID:
17616396
20.

Novel and potent inhibitors of stearoyl-CoA desaturase-1. Part I: Discovery of 3-(2-hydroxyethoxy)-4-methoxy-N-[5-(3-trifluoromethylbenzyl)thiazol-2-yl]benzamide.

Uto Y, Ogata T, Harada J, Kiyotsuka Y, Ueno Y, Miyazawa Y, Kurata H, Deguchi T, Watanabe N, Takagi T, Wakimoto S, Okuyama R, Abe M, Kurikawa N, Kawamura S, Yamato M, Osumi J.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4151-8. doi: 10.1016/j.bmcl.2009.05.119. Epub 2009 Jun 2.

PMID:
19540759

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