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Synthesis and anti-tumor activity of alkenyl camptothecin esters

	author = {Zhi-song CAO and John MENDOZA and Albert DEJESUS and Beppino GIOVANELLA},
	title = {Synthesis and anti-tumor activity of alkenyl camptothecin esters},
	journal = {Acta Pharmacologica Sinica},
	volume = {26},
	number = {2},
	year = {2016},
	keywords = {},
	abstract = {Aim: To study the degrees of influence of changing side ester chains at position C20 of camptothecin on the anti-tumor activity of the molecules. Methods: The
esterification reaction of camptothecin 1 and 9-nitrocamptothecin 2 with crotonic
anhydride in pyridine gave the corresponding esters 3 and 4, respectively. The
acylation of 1 and 2 with cinnamoyl chloride gave products 7 and 8. Epoxidation
reaction of 3 and 4 with m-chloroperoxybenzoic acid in benzene solvent gave the
products 5 and 6. Esters 3, 4, and 5 were tested for anti-tumor activity against 14
human cancer cell lines. Results: Both in vitro and in vivo anti-tumor activity
studies for these esters were conducted and the data demonstrated positive results,
that is, these esters were active against the tested tumor lines. Conclusion: Alkenyl
esters 3 and 4 showed strong anti-tumor activity in vitro against 14 different
cancer cell lines. Ester 3 was active against human breast carcinoma in mice and
the toxicity of the agent was not observed in mice during the treatment, implying
that this agent is effective for treatment with low toxicity.},
	issn = {1745-7254},	url = {}