Synthesis and cytostatic activity of the antitumor antibiotic chartreusin derivatives.

Publisher Website
Google Scholar
Abstract
In order to overcome the rapid biliary excretion of chartreusin, which diminished its activity when administered iv, a series of 3'',4''-O-substituted derivatives of chartreusin were synthesized. Exo-type of 3''4''-O-benzylidene-chartreusin was found active both by ip and iv administration. Therefore, this compound was selected for further modification on its 6-phenol to obtain broader spectra and better pharmacokinetic parameters than the original compound. Several 6-O-acyl-3'',4''-O-exo-benzylidene-chartreusins had high antitumor activity against some murine tumors both by iv and po administration.