2. Academic Validation
  3. Synthesis and cytotoxicity of novel imidazo[4,5-d]azepine compounds derived from marine natural product ceratamine A

Synthesis and cytotoxicity of novel imidazo[4,5-d]azepine compounds derived from marine natural product ceratamine A

  • Bioorg Med Chem Lett. 2018 Mar 1;28(5):866-868. doi: 10.1016/j.bmcl.2018.02.004.
Xuan Pan 1,  Lulu Tao 1,  Ming Ji 1,  Xiaoguang Chen 1,  Zhanzhu Liu 2
Affiliations

Affiliations

  • 1 State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, PR China.
  • 2 State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, PR China. Electronic address: liuzhanzhu@imm.ac.cn.
PMID: 29433924 DOI: 10.1016/j.bmcl.2018.02.004
Abstract

A series of novel imidazo[4,5-d]azepine compounds derived from marine natural product ceratamine A were designed and synthesized in 7 steps. Most compounds exhibited comparable cytotoxicity against five human Cancer cell lines (HCT-116, HepG2, BGC-823, A549 and A2780) to natural product ceratamine A. Compound 1k, bearing methoxy group at C-14, C-15 and C-16, showed the best in vitro cytotoxicity, which was better than ceratamine A. The structure and activity relationships study showed that the benzyloxymethyl group on N-3 played an important role on the cytotoxicity.

Keywords

Anticancer; Ceratamine A; Heck reaction; Microtubule.

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