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Bioorg Med Chem Lett. 2012 Dec 15;22(24):7659-61. doi: 10.1016/j.bmcl.2012.10.002. Epub 2012 Oct 11.

Design and one-pot synthesis of new 7-acyl camptothecin derivatives as potent cytotoxic agents.

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School of Pharmacy, Lanzhou University, Lanzhou 730000, PR China.


New 7-acyl camptothecin derivatives were designed and synthesized from camptothecin in a one-pot reaction through a Minisci type-reaction and were evaluated for cytotoxicity against four tumor cell lines, A-549, DU-145, KB, and KB-vin. All of the new compounds showed significant inhibition of human tumor cell growth, with IC(50) values ranging from 0.01538 to 13.342 μM. Most of the derivatives were more cytotoxic than irinotecan, and the (7a) and 7-propionyl (7b) analogs exhibited the highest cytotoxic activity against the tumor cell lines tested. This compound class merits further development as anticancer clinical trial candidates.

[Indexed for MEDLINE]

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