Exploration of the SAR of anti-invasive chalcones: Synthesis and biological evaluation of conformationally restricted analogues

…, T De Ryck, L Dierickx, BWA Vanhoecke…

Index: Roman, Bart I.; Ryck, Tine De; Dierickx, Laura; Vanhoecke, Barbara W.A.; Katritzky, Alan R.; Bracke, Marc; Stevens, Christian V. Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 15 p. 4812 - 4819

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Citation Number: 16

Abstract

In order to get a clearer view on the active geometry of anti-invasive chalcones, we have prepared a number of isoxazoles and related substances as conformationally restrained mimics of 1, 3-diarylpropenones, and also of (Z)-stilbenes. In vitro anti-invasive activity data for 3, 5-isoxazoles and 4, 5-isoxazoles, together with an in silico geometrical comparison, point towards an active conformation for chalcones more resembling their s-trans ...