Literature DB >> 20570511

Discovery of aminopyridines substituted with benzoxazole as orally active c-Met kinase inhibitors.

Sung Yun Cho1, Sun-Young Han, Jae Du Ha, Jae Wook Ryu, Chong Ock Lee, Heejung Jung, Nam Sook Kang, Hyoung Rae Kim, Jong Sung Koh, Jongkook Lee.   

Abstract

We report the synthesis and biological evaluation of aminopyridines substituted with benzoxazole. The SAR of the aminopyridines was explored to improve the inhibitory activity against c-Met and to decrease hERG affinity. These studies led to the discovery of amide 24 which showed good c-Met inhibitory potency, low affinity to hERG and favorable pharmacokinetic properties in rats. 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20570511     DOI： 10.1016/j.bmcl.2010.05.031

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  6 in total

1.  Pharmacophore modeling and virtual screening studies to identify new c-Met inhibitors.

Authors:  Wenting Tai; Tao Lu; Haoliang Yuan; Fengxiao Wang; Haichun Liu; Shuai Lu; Ying Leng; Weiwei Zhang; Yulei Jiang; Yadong Chen
Journal:  J Mol Model       Date:  2011-12-28       Impact factor: 1.810

2.  Evaluation of a multi-kinase inhibitor KRC-108 as an anti-tumor agent in vitro and in vivo.

Authors:  Sun-Young Han; Chong Ock Lee; Sung-Hoon Ahn; Mi-Ok Lee; So-Young Kang; Hyuk-Jin Cha; Sung Yun Cho; Jae Du Ha; Jae Wook Ryu; Heejung Jung; Hyoung Rae Kim; Jong Sung Koh; Jongkook Lee
Journal:  Invest New Drugs       Date:  2010-11-16       Impact factor: 3.850

3.  (1S,2E,4S,7E,11E)-2,7,11-Cembratriene-4,6-diol semisynthetic analogs as novel c-Met inhibitors for the control of c-Met-dependent breast malignancies.

Authors:  Hassan Y Ebrahim; Mohamed M Mohyeldin; Mohammad M Hailat; Khalid A El Sayed
Journal:  Bioorg Med Chem       Date:  2016-09-13       Impact factor: 3.641

4.  Characterization of KRC-108 as a TrkA Kinase Inhibitor with Anti-Tumor Effects.

Authors:  Hyo Jeong Lee; Yeongyu Moon; Jungil Choi; Jeong Doo Heo; Sekwang Kim; Hari Krishna Nallapaneni; Young-Won Chin; Jongkook Lee; Sun-Young Han
Journal:  Biomol Ther (Seoul)       Date:  2022-03-10       Impact factor: 4.231

5.  Characterization of the aminopyridine derivative KRC-180 as a JAK2 inhibitor.

Authors:  Kyoung Bin Yoon; Sung Yun Cho; Su Jin An; Kyeong Ryang Park; Hyo Jeong Lee; Hae Sung Yoon; Sun-Mi Lee; Yong-Chul Kim; Sun-Young Han
Journal:  Oncol Lett       Date:  2017-06-08       Impact factor: 2.967

6.  Copper-catalyzed synthesis of 2-aminopyridylbenzoxazoles via domino reactions of intermolecular N-arylation and intramolecular O-arylation.

Authors:  Ju-You Lu
Journal:  RSC Adv       Date:  2019-05-01       Impact factor: 4.036
  6 in total

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