Search

A series of 5- C -alkylating camptothecins have been synthesized by one-step method, and their in vitro antitumor activity was evaluated against six human cancer cell lines. The results showed that all 5- C -alkylates of camptothecins possessed poor cytotoxicity on six human cancer cell lines.

A series of heterocyclic acid esters of camptothecins as new compounds had been synthesized by acylation method, their in vitro and in vivo antitumor activities were evaluated. The cytotoxic results showed that 6 possessed the best efficacy on six human cancer cell lines in the six classes of CPTs' derivatives. In vivo testing results indicated that 9 had better antitumor activity against mouse liver carcinoma H22 than topotecan.

A series of heterocycle-substituted phthalimide derivatives were synthesized. Structurally diverse derivatives with heterocyclic rings, including furan, imidazo[1,2-a]pyridine, 1,3,4-thiadiazine, imidazo[2,1-b][1,3,4]thiadiazine, pyrazole, 1,2,4-triazolo[3,4-b][1,3,4]thiadiazine, thiazole and thiazoline, were obtained by the reactions of α-bromoketone intermediate with various nucleophiles containing oxygen, nitrogen and sulfur atom. Their cytotoxic activity was also evaluated against five human cancer cell lines in vitro .