Showing papers by "Beppino C. Giovanella published in 2008"
TL;DR: A simple and sensitive high-performance liquid chromatography assay for the analysis of CZ48, a potent anticancer candidate, and its active metabolite camptothecin (CPT) in mouse plasma was developed and validated and confirmed by the determination of plasma samples in the mice after oral administration of Cz48.
21 citations
TL;DR: The IC50 studies showed that the majority of new aromatic esters of camptothecins 2-29 were not as potent as their parental compounds 1a and 1b; whereas, the potencies of esters 6 and 25 were exceptionally high, much higher than the commercial Camptothecin analogues and comparable to (or slightly more potent than) their parents.
Abstract: Twenty-eight new aromatic esters of camptothecins 2-29 were prepared in yields of 5 to 96% by straight acylation of camptothecin (1a) and 9-nitrocamptothecin (1b) with various aromatic acids as acylating agents. All of these esters were tested against 14 different human cancer cell lines. The antitumor activity of these compounds was related to the nature of the substituting groups of their side aromatic chains. In general, esters with strong electron-withdrawing groups on their side aromatic chains were active; esters with halogen-substituted side aromatic chains were slightly active; and esters without any substituting groups on their side aromatic chains were practically inactive. The IC50 studies showed that the majority of these esters were not as potent as their parental compounds 1a and 1b; whereas, the potencies of esters 6 and 25 were exceptionally high, much higher than the commercial camptothecin analogues and comparable to (or slightly more potent than) their parental compounds.
5 citations