HIF-1α inhibitors: Synthesis and biological evaluation of novel moracin O and P analogues

Y Xia, Y Jin, N Kaur, Y Choi, K Lee

Index: Xia, Yan; Jin, Yinglan; Kaur, Navneet; Choi, Yongseok; Lee, Kyeong European Journal of Medicinal Chemistry, 2011 , vol. 46, # 6 p. 2386 - 2396

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Citation Number: 31

Abstract

Abstract The natural products moracins O and P exhibited potent in vitro inhibitory activity against hypoxia-inducible factor (HIF-1), which is a key mediator during adaptation of cancer cells to tumour hypoxia. Systematic variations of the structures of benzofuran type moracins were made and structure-activity relationship analysis showed the importance of the 2- arylbenzofuran ring and the (R)-configuration of the core scaffold. Further evaluation of the ...