Semi-synthesis and biological activity of gamma-lactones analogs of camptothecin.
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.
Li
Mingzong
M
Department of Chemistry, University of Science & Technology of China, Hefei, Anhui 230026, PR China.
Tang
Weidong
W
Zeng
Fuxing
F
Lou
Liguang
L
You
Tianpa
T
D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000627:therapeutic use; D029769:Camptotheca / Q000378:metabolism; D002166:Camptothecin / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004264:DNA Topoisomerases, Type I / Q000378:metabolism; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020128:Inhibitory Concentration 50; D000077146:Irinotecan; D007783:Lactones / Q000737:chemistry*; D008956:Models, Chemical; D015394:Molecular Structure; D012995:Solubility; D013329:Structure-Activity Relationship
D000972:Antineoplastic Agents, Phytogenic; D007783:Lactones; D000077146:Irinotecan; D004264:DNA Topoisomerases, Type I; D002166:Camptothecin