Structure??activity studies of novel amidine analogues of chlorambucil: Correlation of cytotoxic activity with DNA??binding affinity and topoisomerase II inhibition

A Bielawska, K Bielawski, S Wołczyński…

文献索引：Bielawski, Krzysztof; Bielawska, Anna; Wolczynski, Slawomir Archiv der Pharmazie, 2001 , vol. 334, # 7 p. 235 - 240

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被引用次数: 11

摘要

Abstract A series of amidine analogues of chlorambucil (9—12), where 5-[4-(N-alkylamidino) phenyl]-2-furancarboxamide and the chlorambucil moiety are linked by a NH (CH 2) 2 NH chain, was synthesized and their cytotoxicity has been tested against the growth of human breast cancer MCF-7 cells. Evaluation of the cytotoxicity of compounds 9—12 employing a MTT assay and inhibition of [3 H] thymidine incorporation into DNA demonstrated that ...