609771-42-8Relevant articles and documents
Synthesis and pharmacological evaluation of novel non-lactone analogues of camptothecin
Hautefaye, Patrick,Cimetiere, Bernard,Pierre, Alain,Leonce, Stephane,Hickman, John,Laine, William,Bailly, Christian,Lavielle, Gilbert
, p. 2731 - 2735 (2007/10/03)
Ten novel camptothecin (CPT) derivatives devoid of the lactone function in the E-ring were synthesized and evaluated as anticancer agents. Several of these CPT analogues bearing a five-membered E-ring are potent inhibitors of the DNA relaxation and cleavage reactions catalyzed by topoisomerase I and exhibit promising cytotoxic activities with IC50 values in the nM range. This is the first successful design of lactone-free CPT, providing thus a new avenue to the development of topoisomerase I targeted antitumor agents.