Synthesis of Azaisoflavone Derivatives

• Main Authors: Chin-Tse Chen, 陳欽澤
• Other Authors: Yeh-Long Chen
• Format: Others
• Language: zh-TW
• Published: 2009
• Online Access: http://ndltd.ncl.edu.tw/handle/50674342328224659963

碩士 === 高雄醫學大學 === 醫藥暨應用化學研究所 === 97 === Synthesis and evaluation of azaisoflavone derivatives are described. The synthesis of the main structure is accomplished by using different anilines and β-keto esters in the condensation reaction and Conral-Limpach reaction. We have obtained a number of azaisoflavones substituted with different functional groups for biological evaluations with our aims to investigate structural features with respect to the biological properties and to establish structure-activity relationships (SAR). We expect azaisoflavones can be better than isoflavone compounds in the pharmacological activity and selectivity. Preliminary assays indicated that these compounds were non-cytotoxic against three cancer cells including MCF-7(breast cancer), NCI-H460 (lung cancer) and SF-286 (CNS cancer). Thus, these azaisoflavone derivatives will be evaluated for their anti-osteoporotic activity in the future.