| The Synthesis of Some 17-（2＇-Oxazolyl）-androsta-5,16-diene Deriva-tives as 17α-Hydroxylase／C17,20 -Lyase Inhibitors |
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| 作者姓名： | ZhuNa ZhaoNa LeiXiaoping LingYangzhi VenkatechHundratta AngelaBrodie |
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| 作者单位： | [1]DepartmentofMedicinalChemistry,SchoolofPharmaceuticalSciences,PekingUniversity,Beijing100082 [2]DepartmentofPharmacology＆ExperimentalTherapeutics,SchoolofMedicine,UniversityofMaryland.Baltimore,Maryland21201 |
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| 摘 要： | Several 4‘- and 5‘-substituted 17-(2‘-oxazolyl)-androsta-5,16-diene derivatives were designed and synthesized as inhibitors of 17α-hydroxylase/C17,20 -Lyase (P45017α) for the treatment of prostatic cancer, the results of the preliminary pharmacological screening showed that compound 6c, i.e. 17-(2‘-oxazoly)-androsta-5,16-diene-3-ol was a strong inhibitor, comparable with that of the reference compound VN-85. The introduction ofmethyl or phenyl group at the 4‘ or 5‘ position of oxazole ring decreased the activity. The in vitro activities of 3- acetate 5a-c and 8 were lower than their 3-ol counterparts 6a-c and 9 as expected. The further pharmacological study of 6c is in progress.
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| 关 键 词： | 17-嚼唑基雄甾烯 P45017 抑制剂 前列腺癌 生物电子等排 药理分析 |
The Synthesis of Some 17-(2'-Oxazolyl)-androsta-5,16-diene Derivatives as 17α-Hydroxylase/C17,20-Lyase Inhibitors |
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| ZhuNa ZhaoNa LeiXiaoping LingYangzhi VenkatechHundratta AngelaBrodie.The Synthesis of Some 17-(2'-Oxazolyl)-androsta-5,16-diene Derivatives as 17α-Hydroxylase/C17,20-Lyase Inhibitors[J].Journal of Chinese Pharmaceutical Sciences,2001,10(1):14-19. |
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| Authors: | Zhu Na Zhao Na Lei Xiaoping Ling Yangzhi Venkatech Hundratta Angela Brodie |
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| Abstract: | |
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| Keywords: | 17-Oxazolyl androstene P45017α Inhibitors Prostate cancer Bioisosterism |
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