SYNTHESIS AND EVALUTATION OF CATIONIC ANTITUMOR AGENTS
Project Number1R43CA082949-01A1
Contact PI/Project LeaderWANG, YUQIANG
Awardee OrganizationPANORAMA RESEARCH, INC.
Description
Abstract Text
Malignant cells exhibit increased electronegativity. The mitochondrial membrane
potential is higher in carcinoma cells than in normal epithelial cells. This may be
at least partially responsible for the fact that lipophilic cationic compounds
selectively accumulate in carcinoma cells. We propose to synthesize and
evaluate novel cationic (+)- YW-200 prodrugs. (+)-YW-200 is a new analog of
CC-1065, one of the most potent anticancer drug discovered to date. YW-200 is
1000-fold more potent than doxorubicin against different tumor cell lines in
vitro and shows remarkable antitumor activity in vivo without causing
myelosuppression, the dose-limiting toxicity of other CC-1065 analogs. The new
cationic (+)-YW-200 prodrugs will be water-soluble, selectively taken-up by
cancer cells, and thus have an improved therapeutic index.
PROPOSED COMMERCIAL APPLICATION:
These novel compounds can be used as anticancer drugs.
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