【摘 要】
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Certain 4,5-diarylisoxazole derivatives have been found to possess broad biological effects,including anti-inflammatory and anticancer activities.For example,the cytotoxic combretastatin A-4 can be co
【机 构】
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Department of Medicinal and Applied Chemistry,College of Life Science,Kaohsiung Medical University,K
【出 处】
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第九届IUPAC化学生物学国际研讨会暨第八届世界华人药物化学研讨会
论文部分内容阅读
Certain 4,5-diarylisoxazole derivatives have been found to possess broad biological effects,including anti-inflammatory and anticancer activities.For example,the cytotoxic combretastatin A-4 can be considered as an analogue of 4,5-diarylisoxazole in which the isoxazole moiety was replaced with a simple ethylene bridge.1 Therefore,structural optimization of 4,5-diarylisoxazole could have led to the discovery of potential drug candidates.Recently,we have reported preparation of certain isoflavone derivatives and investigated for their anti-osteoporotic and antiproliferative activities in a detailed SAR study.2 The present report describes the conversion of isoflavones into novel 4,5-diphenylisoxazole derivatives by the treatment with NH2OH.Other synthetic approaches toward 4,5-diphenylisoxazole derivatives have also been reported recently.Alkylation followed by amination of these 4,5-diphenylisoxazoles gave the desired aminoalkoxy substituted 4,5-diphenylisoxazole derivatives.We have discovered that these aminoalkoxy substituted 4,5-diphenylisoxazole derivatives possess potent anti-osteoporotic and/or anticancer activities.
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