Explorative study on the anticancer activity, selectivity and metabolic stability of related analogs of aminosteroid RM-133
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- 作者：Martin Perreaulta ; René ; Maltaisa ; Raphaë ; l Dutoura ; Donald Poiriera ; b ; donald.poirier@crchul.ulaval.ca" class="auth_mail" title="E-mail the corresponding author
- 关键词：Steroid ; Anticancer agent ; Selective cytotoxicity ; Metabolic stability ; Drug
- 刊名：Steroids
- 出版年：2016
- 出版时间：November 2016
- 年：2016
- 卷：115
- 期：Complete
- 页码：105-113
- 全文大小：728 K
文摘
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The aminosteroid RM-133 is a key representative of a new family of anticancer agents.
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Eleven RM-133-related compounds were synthesized and characterized.
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The in vivo potency of RM-133 was improved by protecting its 3α-OH.
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Ester and carbamate derivatives of RM-133 are stabilized against metabolic enzymes.
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The dimethylcarbamate derivative 3 is a selective and more stable anticancer agent.