{"title":"抑制胆固醇侧链切割。第5部分。22-(对氯苯基)胆固醇类似物的合成。","authors":"C P Bergstrom, R Clarke, J F Fitzloff, M C Lu","doi":"","DOIUrl":null,"url":null,"abstract":"<p><p>Three 22-(p-chloroaryl) analogues of cholesterol (6a-c) were synthesized and evaluated as potential inhibitors of the adrenal cholesterol side-chain cleavage enzyme, in comparison with the known 20-aryl analogue, 20-(p-chlorophenyl)-5-prenen-3 beta,20-diol (2b). All were potent inhibitors. An oxygen at C-22 (analogues 6a and 6b) enhanced the strong binding to the enzyme. Two compounds (6b and 6c) are potential substrates of the enzyme. Possible pharmaceutical uses for these compounds and their derivatives are discussed.</p>","PeriodicalId":11271,"journal":{"name":"Drug design and delivery","volume":"7 4","pages":"259-68"},"PeriodicalIF":0.0000,"publicationDate":"1991-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Inhibition of cholesterol side-chain cleavage. Part 5. Synthesis of 22-(p-chlorophenyl) cholesterol analogues.\",\"authors\":\"C P Bergstrom, R Clarke, J F Fitzloff, M C Lu\",\"doi\":\"\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Three 22-(p-chloroaryl) analogues of cholesterol (6a-c) were synthesized and evaluated as potential inhibitors of the adrenal cholesterol side-chain cleavage enzyme, in comparison with the known 20-aryl analogue, 20-(p-chlorophenyl)-5-prenen-3 beta,20-diol (2b). All were potent inhibitors. An oxygen at C-22 (analogues 6a and 6b) enhanced the strong binding to the enzyme. Two compounds (6b and 6c) are potential substrates of the enzyme. Possible pharmaceutical uses for these compounds and their derivatives are discussed.</p>\",\"PeriodicalId\":11271,\"journal\":{\"name\":\"Drug design and delivery\",\"volume\":\"7 4\",\"pages\":\"259-68\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1991-07-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Drug design and delivery\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Drug design and delivery","FirstCategoryId":"1085","ListUrlMain":"","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Inhibition of cholesterol side-chain cleavage. Part 5. Synthesis of 22-(p-chlorophenyl) cholesterol analogues.
Three 22-(p-chloroaryl) analogues of cholesterol (6a-c) were synthesized and evaluated as potential inhibitors of the adrenal cholesterol side-chain cleavage enzyme, in comparison with the known 20-aryl analogue, 20-(p-chlorophenyl)-5-prenen-3 beta,20-diol (2b). All were potent inhibitors. An oxygen at C-22 (analogues 6a and 6b) enhanced the strong binding to the enzyme. Two compounds (6b and 6c) are potential substrates of the enzyme. Possible pharmaceutical uses for these compounds and their derivatives are discussed.
求助内容：
应助结果提醒方式：
京公网安备 11010802042870号
