Synthesis and biological activity of obatoclax derivatives as novel and potent SHP-1 agonists

…, JW Huang, WT Tai, PJ Chen, IK Kim, CW Shiau

Index: Su, Jung-Chen; Chen, Wei-Lin; Liu, Chun-Yu; Shiau, Chung-Wai; Chen, Kuen-Feng; Chen, Pei-Jer; Tai, Wei-Tien; Huang, Jui-Wen; Kim, Inki European Journal of Medicinal Chemistry, 2012 , vol. 56, p. 127 - 133,7

Full Text: HTML

Citation Number: 8

Abstract

Obatoclax is a linear oligopyrrole compound which antagonizes the antiapoptotic effects of the Bcl-2 family. Herein we describe the synthesis of obatoclax derivatives by replacement of the pyrrole and indole ring of obatoclax with thiophene, furan and thiazolidinedione. The in vitro cytotoxicity of the newly synthesized compounds is evaluated against hepatocellular carcinoma cells. Pyrrole and indole substituents of obatoclax analogues exhibited potent ...