2. Academic Validation
  3. Synthesis and biological evaluation of 7-methoxy-1-(3,4,5-trimethoxyphenyl)-4,5-dihydro-2H-benzo[e]indazoles as new colchicine site inhibitors

Synthesis and biological evaluation of 7-methoxy-1-(3,4,5-trimethoxyphenyl)-4,5-dihydro-2H-benzo[e]indazoles as new colchicine site inhibitors

  • Bioorg Med Chem Lett. 2019 Sep 15;29(18):2632-2634. doi: 10.1016/j.bmcl.2019.07.042.
Junhang Jiang 1,  Qingsen Zhang 2,  Jiapeng Guo 1,  Shaoyu Fang 1,  Ruolan Zhou 1,  Ju Zhu 2,  Xin Chen 3,  Youjun Zhou 4,  Canhui Zheng 5
Affiliations

Affiliations

  • 1 School of Biology and Pharmaceutical Engineering, Wuhan Polytechnic University, Wuhan 430023, China; School of Pharmacy, Second Military Medical University, Shanghai 200433, China.
  • 2 School of Pharmacy, Second Military Medical University, Shanghai 200433, China.
  • 3 School of Biology and Pharmaceutical Engineering, Wuhan Polytechnic University, Wuhan 430023, China. Electronic address: chenxin_0001@126.com.
  • 4 School of Pharmacy, Second Military Medical University, Shanghai 200433, China. Electronic address: zhuoyoujun@smmu.edu.cn.
  • 5 School of Pharmacy, Second Military Medical University, Shanghai 200433, China. Electronic address: canhuizheng@smmu.edu.cn.
PMID: 31362922 DOI: 10.1016/j.bmcl.2019.07.042
Abstract

The colchicine site inhibitors (CSIs) displayed both antimitotic and vascular disrupting activities, therefore are promising potential antitumor agents. In this study, a series 1-phenyl-4,5-dihydro-2H-benzo[e]indazoles were found as new CSIs of which the bioactive configuration was locked. Among them, compounds C1 and C2 displayed the best activity, with tubulin polymerization IC50 of 3.4 and 1.5 μM, and growth IC50 of low nanomolar concentrations against human colon Cancer cell lines. In addition, compound C1 showed excellent broad-spectrum antitumor activity in the NCI-60 Human Tumor Cell Lines Screen, encouraging further study of this antitumor compound.

Keywords

Antitumor activity; Colchicine site inhibitors; NCI-60 human tumor cell lines screen; Tubulin polymerization inhibitors.

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