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Semi-synthesis and biological activity of gamma-lactones analogs of camptothecin
Mingzong Li1, Weidong Tang, Fuxing Zeng
1Department of Chemistry, University of Science & Technology of China, Hefei, Anhui 230026, PR China.
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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