Design, synthesis of a novel 4-O-methylsaucerneol analogue LXY7824 as potent HIF-1 inhibitor and anti-cancer agent

Xiao-Yu LiuState Key Laboratory of Bioactive Substance and Function of Natural Medicine, Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing100050, China

Xiao-Yu LiState Key Laboratory of Bioactive Substance and Function of Natural Medicine, Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing100050, China

Fei-Long YangState Key Laboratory of Bioactive Substance and Function of Natural Medicine, Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing100050, China

Yan LiState Key Laboratory of Bioactive Substance and Function of Natural Medicine, Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing100050, China

Xiao-Zhen JiaoState Key Laboratory of Bioactive Substance and Function of Natural Medicine, Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing100050, ChinaCorrespondence[email protected]

Ping XieState Key Laboratory of Bioactive Substance and Function of Natural Medicine, Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing100050, China

Abstract

Hypoxia-inducible factor-1 (HIF-1), an important transcription factor for tumor survival, is an attractive target for anti-cancer treatment. Herein, we present the design and synthesis of LXY7824, a simplified analogue of 4-O-methylsaucerneol. In addition, its significant HIF-1 inhibitory activity and potent anti-cancer activity in vivo and in vitro were also reported.

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Design, synthesis of a novel 4-O-methylsaucerneol analogue LXY7824 as potent HIF-1 inhibitor and anti-cancer agent

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Design, synthesis of a novel 4-O-methylsaucerneol analogue LXY7824 as potent HIF-1 inhibitor and anti-cancer agent

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