Chalcone-based inhibitors against hypoxia-inducible factor 1--structure activity relationship studies

Bioorg Med Chem Lett. 2011 Jan 1;21(1):555-7. doi: 10.1016/j.bmcl.2010.10.063.

Balasubramanian Srinivasan ¹, Thomas E Johnson, Chengguo Xing

Affiliations

Affiliation

1 Department of Medicinal Chemistry, College of Pharmacy, University of Minnesota, 308 Harvard St. SE, Minneapolis MN 55455, United States.

PMID: 21112783 DOI: 10.1016/j.bmcl.2010.10.063

Abstract

Many tumor tissues are under hypoxic conditions. Activating hypoxia-inducible factor 1 (HIF-1), a transcription factor, is a major mechanism for tumor cells to survive and even to evade Other tissues. Therefore inhibiting HIF-1 is a potential strategy to help improve Cancer treatment. Chalcone is a promising template to develop HIF-1 inhibitor because quite a few of chalcone-based compounds reveal moderate HIF-1 inhibitory activity and many chalcone-based compounds demonstrate promising Anticancer activities in various animal models. However, there are no reports about the structure-activity relationship of chalcone compounds with respect to HIF-1 inhibition. This study reports the HIF-1 inhibitory activities of a panel of Chalcones, identifies a few lead candidates of single-digit micromolar potency, and determines important structural modifications.

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