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Small molecule inhibitors of the nuclear translocation of androgen receptor for the treatment of castration-resistant prostate cancer

机译:雄激素受体核转运的小分子抑制剂,用于治疗去势抵抗性前列腺癌

摘要

A compound, or a pharmaceutically acceptable salt or ester thereof, according to formula I:R20—(Z)b—(Y)c—(R21)a—(X)d—R22—R23 wherein R20 is aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a thio-containing group, or a seleno-containing group; Z is alkanediyl, substituted alkanediyl, cycloalkanediyl, or substituted cycloalkanediyl; Y is S, O, S(═O), —S(═O)(═O)—, or NR10, wherein R10 is H or alkyl; R21 is alkanediyl, substituted alkanediyl, cycloalkanediyl, substituted cycloalkanediyl alkadienyl, substituted alkadienyl, alkatrienyl, substituted alkatrienyl; X is —C(═O)—, —S(═O)(═O)—, or —N(H)C(═O)—; R22 includes at least one divalent amino radical; R23 is aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a thio-containing group, or a seleno-containing group; a, b, c, and d independently are 0 or 1.
机译:根据式I的化合物或其药学上可接受的盐或酯:<?in-line-formulae description =“ In-line Formulae” end =“ lead”?> R 20 &#x2014;(Z) b &#x2014; (Y) c &#x2014;(R 21 a &#x2014;(X) d & #x2014; R 22 &#x2014; R 23 <?in-line-formulae description =“ In-line Formulae” end =“ tail”?>其中R 20表示芳基,取代的芳基,杂芳基,取代的杂芳基,杂环烷基,取代的杂环烷基,烷氧基,芳氧基,含硫基团或含硒基团; Z为烷二基,取代的烷二基,环烷二基或取代的环烷二基; Y是S,O,S(&#x2550; O),&#x2014; S(&#x2550; O)(&#x2550; O)&#x2014;或NR 10 ,其中R 10 是H或烷基; R 21代表链烷二基,取代的链烷二基,环链烷二基,取代的环烷二基链二烯基,取代的链二烯基,烷三烯基,取代的链烷三烯基; X是&#x2014; C(&#x2550; O)&#x2014 ;、&#x2014; S(&#x2550; O)(&#x2550; O)&#x2014;或&#x2014; N( H)C(&#x2550; O)&#x2014 ;; R 22 包括至少一个二价氨基; R 23表示芳基,取代的芳基,杂芳基,取代的杂芳基,杂环烷基,取代的杂环烷基,烷氧基,芳氧基,含硫基或含硒基; a,b,c和d分别为0或1。

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