Convenient Synthesis and Biological Evaluation of Bis(indolyl)methane Alkaloid and Bis(aryl)alkanes Derivatives with Anti-cancer Properties  

  1. Liang QiORCID Logo,
  2. Linxia Xiao and
  3. Rui Lin

Submitting author affiliation: JiangSu Vocational College of Medicine, Yancheng, China

Beilstein Arch. 2020, 202060.

Published 08 May 2020

  • Preprint


An efficient and metal free methodology for the synthesis of bis(indolyl)methanes (BIMs) and bis(aryl)alkanes derivatives in the presence of B(C6F5)3 by the condensation of primary amines with pyruvates with good to high yields have been successfully developed. Some BIMs derivatives displayed good in vitro antitumor activity, screened by MTT assay. Compound 3b show the best anti-cancer activity against lung carcinoma cell A549 cells with IC50 of 4.52 µM.

Keywords: bis(indolyl)methanes derivatives; metal free; primary amines; pyruvates; antitumor

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Qi, L.; Xiao, L.; Lin, R. Beilstein Arch. 2020, 202060. doi:10.3762/bxiv.2020.60.v1

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