Synthesis, biological evaluation, 3D-QSAR studies of novel aryl-2H-pyrazole derivatives as telomerase inhibitors

Y Luo, S Zhang, KM Qiu, ZJ Liu, YS Yang, J Fu…

Index: Luo, Yin; Zhang, Shuai; Qiu, Ke-Ming; Liu, Zhi-Jun; Yang, Yu-Shun; Fu, Jie; Zhong, Wei-Qing; Zhu, Hai-Liang Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 4 p. 1091 - 1095

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Citation Number: 13

Abstract

A series of novel aryl-2H-pyrazole derivatives bearing 1, 4-benzodioxan or 1, 3- benzodioxole moiety were designed as potential telomerase inhibitors to enhance the ability of aryl-2H-pyrazole derivatives to inhibit telomerase, a target of anticancer. The telomerase inhibition tests showed that compound 16A displayed the most potent inhibitory activity with IC50 value of 0.9 μM for telomerase. The antiproliferative tests showed that compound ...