7-Cycloalkylcamptothecin derivatives: Preparation and biological evaluation

  • Bioorg Med Chem Lett. 2009 Aug 1;19(15):4107-9. doi: 10.1016/j.bmcl.2009.06.010.
Mingzong Li  1 ,  Wei Jin ,  Chen Jiang ,  Chao Zheng ,  Weidong Tang ,  Tianpa You ,  Liguang Lou
Affiliations
  • 1. Department of Chemistry, University of Science & Technology of China, Hefei, Anhui 230026, PR China.
PMID: 19541483 DOI: 10.1016/j.bmcl.2009.06.010
Abstract

A series of 7-cycloalkylcamptothecin derivatives were synthesized from camptothecin with two methods. Their biological activities in vitro were evaluated with sulforhodamine-B (SRB) method on four types of human tumor cell lines A549/ATCC, HT29, NCI-H460 and HL60. Most of these camptothecin analogues show higher antitumor activity than the reference compounds SN-38 and Topotecan, with the IC(50) values low to nM level. Structure-activity relationship studies of these compounds mostly match the conclusion we achieved before from quantitative structure-activity relationship (QSAR) research.