Tropolones as lead-like natural products: the development of potent and selective histone deacetylase inhibitors

SN Ononye, MD VanHeyst, EZ Oblak…

Index: Ononye, Sophia N.; Vanheyst, Michael D.; Oblak, E. Zachary; Zhou, Wangda; Ammar, Mohamed; Anderson, Amy C.; Wright, Dennis L. ACS Medicinal Chemistry Letters, 2013 , vol. 4, # 8 p. 757 - 761

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Citation Number: 27

Abstract

Natural products have long been recognized as a rich source of potent therapeutics but further development is often limited by high structural complexity and high molecular weight. In contrast, at the core of the thujaplicins is a lead-like tropolone scaffold characterized by relatively low molecular weight, ample sites for diversification, and metal-binding functionality poised for targeting a range of metalloenzyme drug targets. Here, we ...