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…

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

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Citation Number: 11

Abstract

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 ...

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Discovery and biological evaluation of 5-aryl-2-furfuramides...

[Kort, Michael E.; Drizin, Irene; Gregg, Robert J.; Scanio, Marc J. C.; Shi, Lei; Gross, Michael F.; Atkinson, Robert N.; Johnson, Matthew S.; Pacofsky, Gregory J.; Thomas, James B.; Carroll, William A.; Krambis, Michael J.; Liu, Dong; Shieh, Char-Chang; Zhang, XuFeng; Hernandez, Gricelda; Mikusa, Joseph P.; Zhong, Chengmin; Joshi, Shailen; Honore, Prisca; Roeloffs, Rosemarie; Marsh, Kennan C.; Murray, Bernard P.; Liu, Jinrong; Werness, Stephen; Faltynek, Connie R.; Krafte, Douglas S.; Jarvis, Michael F.; Chapman, Mark L.; Marron, Brian E. Journal of Medicinal Chemistry, 2008 , vol. 51, # 3 p. 407 - 416]