Synthesis and biological activity of C-7, C-9 and C-10 modified taxane analogues from 1-deoxybaccatin VI

  • Bioorg Med Chem. 2020 Nov 1;28(21):115736. doi: 10.1016/j.bmc.2020.115736.
Chenghu Xie  1 ,  Yongmei Cui  1 ,  Lanlan Li  2 ,  Minmin Zhang  2 ,  Hongchun Liu  3 ,  Haixia Lin  4
Affiliations
  • 1. Department of Chemistry, Innovative Drug Research Center, College of Sciences, Shanghai University, Shanghai, China.
  • 2. Division of Anti-tumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China.
  • 3. Division of Anti-tumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China. Electronic address: [email protected].
  • 4. Department of Chemistry, Innovative Drug Research Center, College of Sciences, Shanghai University, Shanghai, China. Electronic address: [email protected].
PMID: 33065439 DOI: 10.1016/j.bmc.2020.115736
Abstract

A series of C-7, C-9 and C-10 modified taxane analogues were synthesized and their in vitro Anticancer activities against three human Cancer cell lines: A-549 (human lung Cancer cell line), MDA-MB-231 (human breast Cancer cell line), A-549/T (human lung Cancer resistant cell line) were studied. The novel 1-deoxybaccatin VI derivatives modified with carbonate group at C-9 and C-10 positions enable the behavior of these compounds to be evidently distinct from Other similar compounds. The strong cytotoxicity in the three cell lines, especially in drug-resistant cell line, showed by the newly synthesized taxane analogues indicated them as potential lead compounds for Anticancer drug design.

Keywords
1-Deoxybaccatin VI; In vitro anticancer activity; Paclitaxel; Synthesis; Taxane analogues.