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Results: 1 to 20 of 102

1.

Synthesis and biological evaluation of 2-benzylamino-4(5)-(6-methylpyridin-2-yl)-5(4)-([1,2,4]triazolo[1,5-a]-pyridin-6-yl)thiazoles as transforming growth factor-β type 1 receptor kinase inhibitors.

Krishnaiah M, Jin CH, Sreenu D, Subrahmanyam VB, Rao KS, Son DH, Park HJ, Kim SW, Sheen YY, Kim DK.

Eur J Med Chem. 2012 Nov;57:74-84. doi: 10.1016/j.ejmech.2012.09.011. Epub 2012 Sep 20.

PMID:
23047226
[PubMed - indexed for MEDLINE]
2.

Synthesis and biological evaluation of 1-substituted-3-(6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors.

Jin CH, Krishnaiah M, Sreenu D, Subrahmanyam VB, Rao KS, Mohan AV, Park CY, Son JY, Sheen YY, Kim DK.

Bioorg Med Chem Lett. 2011 Oct 15;21(20):6049-53. doi: 10.1016/j.bmcl.2011.08.064. Epub 2011 Aug 22.

PMID:
21911290
[PubMed - indexed for MEDLINE]
3.

Synthesis and biological evaluation of 5-(pyridin-2-yl)thiazoles as transforming growth factor-beta type1 receptor kinase inhibitors.

Kim DK, Choi JH, An YJ, Lee HS.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):2122-7. doi: 10.1016/j.bmcl.2008.01.084. Epub 2008 Jan 30.

PMID:
18262787
[PubMed - indexed for MEDLINE]
4.

Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinolin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors.

Jin CH, Krishnaiah M, Sreenu D, Rao KS, Subrahmanyam VB, Park CY, Son JY, Sheen YY, Kim DK.

Bioorg Med Chem. 2011 Apr 15;19(8):2633-40. doi: 10.1016/j.bmc.2011.03.008. Epub 2011 Mar 22.

PMID:
21435890
[PubMed - indexed for MEDLINE]
5.

Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors.

Jin CH, Sreenu D, Krishnaiah M, Subrahmanyam VB, Rao KS, Nagendra Mohan AV, Park CY, Son JY, Son DH, Park HJ, Sheen YY, Kim DK.

Eur J Med Chem. 2011 Sep;46(9):3917-25. doi: 10.1016/j.ejmech.2011.05.063. Epub 2011 Jun 22.

PMID:
21696866
[PubMed - indexed for MEDLINE]
6.

Synthesis and biological evaluation of 4(5)-(6-methylpyridin-2-yl)imidazoles and -pyrazoles as transforming growth factor-beta type 1 receptor kinase inhibitors.

Kim DK, Lee YI, Lee YW, Dewang PM, Sheen YY, Kim YW, Park HJ, Yoo J, Lee HS, Kim YK.

Bioorg Med Chem. 2010 Jun 15;18(12):4459-67. doi: 10.1016/j.bmc.2010.04.071. Epub 2010 Apr 28.

PMID:
20472445
[PubMed - indexed for MEDLINE]
7.

Synthesis and biological evaluation of benzenesulfonamide-substituted 4-(6-alkylpyridin-2-yl)-5-(quinoxalin-6-yl)imidazoles as transforming growth factor-beta type 1 receptor kinase inhibitors.

Kim DK, Jung SH, Lee HS, Dewang PM.

Eur J Med Chem. 2009 Feb;44(2):568-76. doi: 10.1016/j.ejmech.2008.03.024. Epub 2008 Apr 4.

PMID:
18467006
[PubMed - indexed for MEDLINE]
8.

Synthesis and biological evaluation of 4(5)-(6-alkylpyridin-2-yl)imidazoles as transforming growth factor-beta type 1 receptor kinase inhibitors.

Kim DK, Jang Y, Lee HS, Park HJ, Yoo J.

J Med Chem. 2007 Jun 28;50(13):3143-7. Epub 2007 Jun 7.

PMID:
17552507
[PubMed - indexed for MEDLINE]
9.

Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/antifibrotic agent.

Jin CH, Krishnaiah M, Sreenu D, Subrahmanyam VB, Rao KS, Lee HJ, Park SJ, Park HJ, Lee K, Sheen YY, Kim DK.

J Med Chem. 2014 May 22;57(10):4213-38. doi: 10.1021/jm500115w. Epub 2014 May 13.

PMID:
24786585
[PubMed - indexed for MEDLINE]
10.

Synthesis and biological evaluation of 1-(6-methylpyridin-2-yl)-5-(quinoxalin-6-yl)-1,2,3-triazoles as transforming growth factor-β type 1 receptor kinase inhibitors.

Li F, Park Y, Hah JM, Ryu JS.

Bioorg Med Chem Lett. 2013 Feb 15;23(4):1083-6. doi: 10.1016/j.bmcl.2012.12.008. Epub 2012 Dec 20.

PMID:
23294702
[PubMed - indexed for MEDLINE]
11.

4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-5(3)-(6-methylpyridin-2-yl)imidazole and -pyrazole derivatives as potent and selective inhibitors of transforming growth factor-β type I receptor kinase.

Jin CH, Krishnaiah M, Sreenu D, Subrahmanyam VB, Park HJ, Park SJ, Sheen YY, Kim DK.

Bioorg Med Chem. 2014 May 1;22(9):2724-32. doi: 10.1016/j.bmc.2014.03.022. Epub 2014 Mar 21.

PMID:
24704197
[PubMed - in process]
12.

Design, synthesis, and evaluation of novel 4-thiazolylimidazoles as inhibitors of transforming growth factor-β type I receptor kinase.

Amada H, Sekiguchi Y, Ono N, Matsunaga Y, Koami T, Asanuma H, Shiozawa F, Endo M, Ikeda A, Aoki M, Fujimoto N, Wada R, Sato M.

Bioorg Med Chem Lett. 2012 Mar 1;22(5):2024-9. doi: 10.1016/j.bmcl.2012.01.066. Epub 2012 Jan 28.

PMID:
22325945
[PubMed - indexed for MEDLINE]
13.

Synthesis and biological evaluation of 1,2,4-trisubstituted imidazoles as inhibitors of transforming growth factor-β type I receptor (ALK5).

Guo C, Zhang C, Li X, Li W, Xu Z, Bao L, Ding Y, Wang L, Li S.

Bioorg Med Chem Lett. 2013 Nov 1;23(21):5850-4. doi: 10.1016/j.bmcl.2013.08.105. Epub 2013 Sep 5.

PMID:
24055046
[PubMed - indexed for MEDLINE]
14.

Synthesis and biological evaluation of 2-pyridyl-substituted pyrazoles and imidazoles as transforming growth factor-beta type 1 receptor kinase inhibitors.

Dewang PM, Kim DK.

Bioorg Med Chem Lett. 2010 Jul 15;20(14):4228-32. doi: 10.1016/j.bmcl.2010.05.032. Epub 2010 May 15.

PMID:
20621731
[PubMed - indexed for MEDLINE]
15.

EW-7203, a novel small molecule inhibitor of transforming growth factor-β (TGF-β) type I receptor/activin receptor-like kinase-5, blocks TGF-β1-mediated epithelial-to-mesenchymal transition in mammary epithelial cells.

Park CY, Kim DK, Sheen YY.

Cancer Sci. 2011 Oct;102(10):1889-96. doi: 10.1111/j.1349-7006.2011.02014.x. Epub 2011 Jul 29.

PMID:
21707864
[PubMed - indexed for MEDLINE]
16.

EW-7195, a novel inhibitor of ALK5 kinase inhibits EMT and breast cancer metastasis to lung.

Park CY, Son JY, Jin CH, Nam JS, Kim DK, Sheen YY.

Eur J Cancer. 2011 Nov;47(17):2642-53. doi: 10.1016/j.ejca.2011.07.007. Epub 2011 Aug 16.

PMID:
21852112
[PubMed - indexed for MEDLINE]
17.

5-(1,3-Benzothiazol-6-yl)-4-(4-methyl-1,3-thiazol-2-yl)-1H-imidazole derivatives as potent and selective transforming growth factor-β type I receptor inhibitors.

Amada H, Sekiguchi Y, Ono N, Koami T, Takayama T, Yabuuchi T, Katakai H, Ikeda A, Aoki M, Naruse T, Wada R, Nozoe A, Sato M.

Bioorg Med Chem. 2012 Dec 15;20(24):7128-38. doi: 10.1016/j.bmc.2012.09.066. Epub 2012 Oct 12.

PMID:
23117174
[PubMed - indexed for MEDLINE]
18.

Synthesis and biological evaluation of novel 2-pyridinyl-[1,2,3]triazoles as inhibitors of transforming growth factor beta 1 type 1 receptor.

Kim DK, Kim J, Park HJ.

Bioorg Med Chem Lett. 2004 May 17;14(10):2401-5.

PMID:
15109621
[PubMed - indexed for MEDLINE]
19.

Synthesis and biological evaluation of 1,2,4-trisubstituted imidazoles and 1,3,5-trisubstituted pyrazoles as inhibitors of transforming growth factor beta type 1 receptor (ALK5).

Li X, Wang L, Long L, Xiao J, Hu Y, Li S.

Bioorg Med Chem Lett. 2009 Aug 15;19(16):4868-72. doi: 10.1016/j.bmcl.2009.04.066. Epub 2009 Apr 20.

PMID:
19616940
[PubMed - indexed for MEDLINE]
20.

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
[PubMed - indexed for MEDLINE]

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