2. Academic Validation
  3. Identification and synthesis of N'-(2-oxoindolin-3-ylidene)hydrazide derivatives against c-Met kinase

Identification and synthesis of N'-(2-oxoindolin-3-ylidene)hydrazide derivatives against c-Met kinase

  • Bioorg Med Chem Lett. 2011 Jun 15;21(12):3749-54. doi: 10.1016/j.bmcl.2011.04.064.
Zhongjie Liang 1,  Dengyou Zhang,  Jing Ai,  Limin Chen,  Hengshuai Wang,  Xiangqian Kong,  Mingyue Zheng,  Hong Liu,  Cheng Luo,  Meiyu Geng,  Hualiang Jiang,  Kaixian Chen
Affiliations

Affiliation

  • 1 Drug Discovery and Design Center, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China.
PMID: 21561768 DOI: 10.1016/j.bmcl.2011.04.064
Abstract

A series of N'-(2-oxoindolin-3-ylidene)hydrazide derivatives were identified as moderately potent inhibitors against c-Met kinase by pharmacophore-based virtual screening and chemical synthesis methods. The structure-activity relationship (SAR) at various positions of the scaffold was investigated and its binding mode with c-Met kinase was analyzed by molecular modeling studies. In this study, two potent compounds D2 and D25, with IC(50) value at 1.3 μM and 2.2 μM against c-Met kinase respectively, were identified. Finally, based on the clues extracted from this study, future development for the optimization of this scaffold was discussed.

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