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Items: 1 to 20 of 179

1.

Discovery of novel imidazo[1,2-a]pyridines as inhibitors of the insulin-like growth factor-1 receptor tyrosine kinase.

Ducray R, Simpson I, Jung FH, Nissink JW, Kenny PW, Fitzek M, Walker GE, Ward LT, Hudson K.

Bioorg Med Chem Lett. 2011 Aug 15;21(16):4698-701. doi: 10.1016/j.bmcl.2011.06.093. Epub 2011 Jun 29.

PMID:
21775140
2.

Novel imidazo[1,2-a]pyridine based inhibitors of the IGF-1 receptor tyrosine kinase: optimization of the aniline.

Ducray R, Jones CD, Jung FH, Simpson I, Curwen J, Pass M.

Bioorg Med Chem Lett. 2011 Aug 15;21(16):4702-4. doi: 10.1016/j.bmcl.2011.06.090. Epub 2011 Jun 25.

PMID:
21764307
3.

Discovery of 3,5-disubstituted-1H-pyrrolo[2,3-b]pyridines as potent inhibitors of the insulin-like growth factor-1 receptor (IGF-1R) tyrosine kinase.

Patnaik S, Stevens KL, Gerding R, Deanda F, Shotwell JB, Tang J, Hamajima T, Nakamura H, Leesnitzer MA, Hassell AM, Shewchuck LM, Kumar R, Lei H, Chamberlain SD.

Bioorg Med Chem Lett. 2009 Jun 1;19(11):3136-40. doi: 10.1016/j.bmcl.2008.12.110. Epub 2009 Jan 6.

PMID:
19394223
4.

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
5.

IRAK-4 inhibitors. Part III: a series of imidazo[1,2-a]pyridines.

Buckley GM, Fosbeary R, Fraser JL, Gowers L, Higueruelo AP, James LA, Jenkins K, Mack SR, Morgan T, Parry DM, Pitt WR, Rausch O, Richard MD, Sabin V.

Bioorg Med Chem Lett. 2008 Jun 15;18(12):3656-60. doi: 10.1016/j.bmcl.2008.04.042. Epub 2008 Apr 24.

PMID:
18501603
6.

Discovery and SAR of thiazolidine-2,4-dione analogues as insulin-like growth factor-1 receptor (IGF-1R) inhibitors via hierarchical virtual screening.

Liu X, Xie H, Luo C, Tong L, Wang Y, Peng T, Ding J, Jiang H, Li H.

J Med Chem. 2010 Mar 25;53(6):2661-5. doi: 10.1021/jm901798e.

PMID:
20178321
7.

Novel 2-phenylquinolin-7-yl-derived imidazo[1,5-a]pyrazines as potent insulin-like growth factor-I receptor (IGF-IR) inhibitors.

Mulvihill MJ, Ji QS, Coate HR, Cooke A, Dong H, Feng L, Foreman K, Rosenfeld-Franklin M, Honda A, Mak G, Mulvihill KM, Nigro AI, O'Connor M, Pirrit C, Steinig AG, Siu K, Stolz KM, Sun Y, Tavares PA, Yao Y, Gibson NW.

Bioorg Med Chem. 2008 Feb 1;16(3):1359-75. Epub 2007 Oct 23.

PMID:
17983756
8.

Design and biological evaluation of imidazo[1,2-a]pyridines as novel and potent ASK1 inhibitors.

Terao Y, Suzuki H, Yoshikawa M, Yashiro H, Takekawa S, Fujitani Y, Okada K, Inoue Y, Yamamoto Y, Nakagawa H, Yao S, Kawamoto T, Uchikawa O.

Bioorg Med Chem Lett. 2012 Dec 15;22(24):7326-9. doi: 10.1016/j.bmcl.2012.10.084. Epub 2012 Oct 23.

PMID:
23147077
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.

J Med Chem. 2009 Dec 10;52(23):7360-3. doi: 10.1021/jm900786r.

PMID:
19778024
10.

A novel, potent, and selective insulin-like growth factor-I receptor kinase inhibitor blocks insulin-like growth factor-I receptor signaling in vitro and inhibits insulin-like growth factor-I receptor dependent tumor growth in vivo.

Ji QS, Mulvihill MJ, Rosenfeld-Franklin M, Cooke A, Feng L, Mak G, O'Connor M, Yao Y, Pirritt C, Buck E, Eyzaguirre A, Arnold LD, Gibson NW, Pachter JA.

Mol Cancer Ther. 2007 Aug;6(8):2158-67. Epub 2007 Aug 1.

11.

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.

J Med Chem. 2005 Sep 8;48(18):5639-43.

PMID:
16134929
12.

Synthesis and biological evaluation of imidazo[1,2-a]pyridine derivatives as novel PI3 kinase p110alpha inhibitors.

Hayakawa M, Kaizawa H, Kawaguchi K, Ishikawa N, Koizumi T, Ohishi T, Yamano M, Okada M, Ohta M, Tsukamoto S, Raynaud FI, Waterfield MD, Parker P, Workman P.

Bioorg Med Chem. 2007 Jan 1;15(1):403-12. Epub 2006 Oct 16.

PMID:
17049248
13.

Synthesis and SAR of 2-phenoxypyridines as novel c-Jun N-terminal kinase inhibitors.

Song X, Chen W, Lin L, Ruiz CH, Cameron MD, Duckett DR, Kamenecka TM.

Bioorg Med Chem Lett. 2011 Dec 1;21(23):7072-5. doi: 10.1016/j.bmcl.2011.09.090. Epub 2011 Sep 29.

PMID:
22004719
14.

Discovery and evaluation of 3-phenyl-1H-5-pyrazolylamine-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).

Lin WH, Hsieh SY, Yen SC, Chen CT, Yeh TK, Hsu T, Lu CT, Chen CP, Chen CW, Chou LH, Huang YL, Cheng AH, Chang YI, Tseng YJ, Yen KR, Chao YS, Hsu JT, Jiaang WT.

Bioorg Med Chem. 2011 Jul 15;19(14):4173-82. doi: 10.1016/j.bmc.2011.06.016. Epub 2011 Jun 13.

PMID:
21708468
15.

Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors.

Hayakawa M, Kawaguchi K, Kaizawa H, Koizumi T, Ohishi T, Yamano M, Okada M, Ohta M, Tsukamoto S, Raynaud FI, Parker P, Workman P, Waterfield MD.

Bioorg Med Chem. 2007 Sep 1;15(17):5837-44. Epub 2007 Jun 6.

PMID:
17601739
16.

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
17.

Design, synthesis, and evaluation of novel VEGFR2 kinase inhibitors: discovery of [1,2,4]triazolo[1,5-a]pyridine derivatives with slow dissociation kinetics.

Oguro Y, Cary DR, Miyamoto N, Tawada M, Iwata H, Miki H, Hori A, Imamura S.

Bioorg Med Chem. 2013 Aug 1;21(15):4714-29. doi: 10.1016/j.bmc.2013.04.042. Epub 2013 Apr 23.

PMID:
23755884
18.

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
19.

Rapid generation of a high quality lead for transforming growth factor-beta (TGF-beta) type I receptor (ALK5).

Goldberg FW, Ward RA, Powell SJ, Debreczeni JE, Norman RA, Roberts NJ, Dishington AP, Gingell HJ, Wickson KF, Roberts AL.

J Med Chem. 2009 Dec 10;52(23):7901-5. doi: 10.1021/jm900807w.

PMID:
19736928
20.

Design and synthesis of 3-(4,5,6,7-tetrahydro-3H-imidazo[4,5-c]pyridin-2-yl)-1H-quinolin-2-ones as VEGFR-2 kinase inhibitors.

Han SY, Choi JW, Yang J, Chae CH, Lee J, Jung H, Lee K, Ha JD, Kim HR, Cho SY.

Bioorg Med Chem Lett. 2012 Apr 15;22(8):2837-42. doi: 10.1016/j.bmcl.2012.02.073. Epub 2012 Mar 7.

PMID:
22450128

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