Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 52, Issue 4, Pages 1029-1039Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm801153y
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The synthesis, biological activity, and molecular modeling studies of C-ring-rnodified camptothecins are reported. A general synthetic protocol, based on C-5 camptothecin (C-5-CPT) enolate chemistry, allows one to obtain various C5-substituted analogues. All new Compounds, obtained as 1:1 epimeric mixtures, were tested for their antiproliferative activity. Experimental data showed that all novel derivatives are less active than the reference compounds and that one of the two epimers; is more active than the other. Molecular docking simulations were performed to achieve more insight into the interactions between the new C5-modified CPTs and Topo I. A good correlation was observed when the data of cytotoxicity and the values calculated for the free binding energy were combined.
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