Synthesis of novel 17-(4′-formyl)pyrazolylandrosta-5,16-dienes and their derivatives as potent 17α-hydroxylase/C17,20-lyase inhibitors or antiproliferative agents depending on the substitution pattern of the heteroring
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- 作者：Dó ; ra Ková ; csa ; Já ; nos Wö ; lflinga ; Nikoletta Szabó ; b ; Mihá ; ly Szé ; csib ; Zsuzsanna Schelzc ; Istvá ; n Zupkó ; c ; É ; va Franka ; frank@chem.u-szeged.hu" class="auth_mail" title="E-mail the corresponding author
- 关键词：Steroids ; Vilsmeier-Haack formylation ; Pyrazoles ; Antiproliferative effect ; C17 ; 20-lyase inhibition
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：14 September 2016
- 年：2016
- 卷：120
- 期：Complete
- 页码：284-295
- 全文大小：531 K
文摘
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A series of novel 17-(4′-formyl)pyrazolylandrosta-5,16-dienes were efficiently synthesized.
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Cyclization/formylation of steroidal hydrazones were carried out under Vilsmeier conditions.
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Derivatization of the primary products led to a large set of structurally diverse compounds.
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Several derivatives exerted substantial effects on cell proliferation.
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Three of the tested pyrazoles displayed noteworthy inhibition on rat testicular C17,20-lyase.