一类苄基咔唑衍生物的合成及其芳香化酶抑制活性  

Synthesis and Aromatase Inhibitory Activities of Some Benzyl Carbazole Derivatives

作　　者：戴玉杰[1] 刘艳春 孙紫悦 宋智丹 刘伟[2] 张秀利[1] DAI Yujie;LIU Yanchun;SUN Ziyue;SONG Zhidan;LIU Wei;ZHANG Xiuli(Key Laboratory of Industrial Fermentation Microbiology,Ministry of Education,College of Biotechnology, Tianjin University of Science & Technology,Tianjin 300457,China;College of Science,Tianjin University of Science & Technology,Tianjin 300457,China)

机构地区：[1]工业发酵微生物教育部重点实验室,天津科技大学生物工程学院,天津300457 [2]天津科技大学理学院,天津300457

出　　处：《天津科技大学学报》2017年第4期20-23,35,共5页Journal of Tianjin University of Science & Technology

基　　金：国家自然科学基金资助项目(21272171)

摘　　要：许多含咔唑结构的天然产物和药物分子具有广泛的生物和药理活性.在前期研究中发现苄基咔唑类化合物具有芳香化酶抑制活性的基础上,合成10个苄基咔唑衍生物(其中,前7个化合物是未被文献报道过的化合物),采用1H NMR确证它们的结构,在体外酶水平上测定它们对芳香化酶的抑制活性,并总结取代基对其活性影响的构效关系.该研究可为进一步寻找更高活性苄基咔唑类芳香化酶抑制剂提供基础数据和思路.Many natural substances and drug molecules with the carbazole structure have a broad range of biological and pharmacological activities.Based on our previous discovery that benzyl carbazole possesses aromatase inhibitory activity,ten substitutes were synthesized(the first seven compounds are unreported in literature),and their structure was confirmed by1H NMR.Their aromatase inhibitory activities were assayed in vitro at enzyme levels and the structure activity relationship was summarized.This research can provide some basic data and ideas for the further search of new benzyl carbazole derivatives with higher aromatase inhibitory activities.

关 键 词：苄基咔唑衍生物 合成 芳香化酶抑制剂 

分 类 号：R914.5[医药卫生—药物化学]