2. Academic Validation
  3. Semi-synthesis and biological activity of gamma-lactones analogs of camptothecin

Semi-synthesis and biological activity of gamma-lactones analogs of camptothecin

  • Bioorg Med Chem Lett. 2008 Dec 15;18(24):6441-3. doi: 10.1016/j.bmcl.2008.10.074.
Mingzong Li 1,  Weidong Tang,  Fuxing Zeng,  Liguang Lou,  Tianpa You
Affiliations

Affiliation

  • 1 Department of Chemistry, University of Science & Technology of China, Hefei, Anhui 230026, PR China.
PMID: 18986807 DOI: 10.1016/j.bmcl.2008.10.074
Abstract

A series of E-ring gamma-lactone camptothecin derivatives were synthesized by semi-synthesis via a three-step domino reaction. Their biological activity was evaluated on two types of human tumor cell lines A549 and HT-29 with sulforhodamine-B (SRB) method. The antitumor activity of these compounds was lower than SN-38, only compound 12c was found to be close to the activity of Topotecan. The structure-activity relationship (SAR) of these analogs was studied and discussed.

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