Ontology highlight
ABSTRACT:
SUBMITTER: Moon SJ
PROVIDER: S-EPMC2661425 | biostudies-literature | 2008 Nov
REPOSITORIES: biostudies-literature
Moon Sung-Ju SJ Govindan Serengulam V SV Cardillo Thomas M TM D'Souza Christopher A CA Hansen Hans J HJ Goldenberg David M DM
Journal of medicinal chemistry 20081022 21
CPT-11 is a clinically used cancer drug, and it is a prodrug of the potent topoisomerase I inhibitor, SN-38 (7-ethyl-10-hydroxycamptothecin). To bypass the need for the in vivo conversion of CPT-11 and increase the therapeutic index, bifunctional derivatives of SN-38 were prepared for use in antibody-based targeted therapy of cancer. The general synthetic scheme incorporated an acetylene-azide click cycloaddition step in the design, a short polyethylene glycol spacer for aqueous solubility, and ...[more]