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SMALL MOLECULE INHIBITORS OF THE NUCLEAR TRANSLOCATION OF ANDROGEN RECEPTOR FOR THE TREATMENT OF CASTRATION-RESISTANT PROSTATE CANCER

机译:小分子抑制剂的雄激素受体核易位治疗抗阉割前列腺癌

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, cycloalkyl, substituted cycloalkyl, 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, cycloalkenediyl, substituted cycloalkenediyl, 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, cycloalkyl, substituted cycloalkyl, 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:R20-(Z)B-(Y)C-(R21)A-(X)D-R22-R23,其中R 2 O是芳基,取代芳基,其中α(x)的化合物或其药学上可接受的盐或酯杂芳基,取代的杂芳基,环烷基,取代的环烷基,杂环烷基,取代的杂环烷基,烷氧基,芳氧基,含硫氧脲基团; Z是链烷基二基,取代的链烷基,环烷基二酯或取代的环烷烷基苯基; Y是S,O,S(= O),-S(= O)(= O) - 或NR10,其中R10是H或烷基; R21是链烷基,取代的链烷基,环烷基二基,取代的环烷基二基,链烷基,取代的链烷基,环己烷基,取代的环己烷二基,烷基苯基,取代的allatrienyl; x是-c(= o) - ,-s(= o)(= o) - ,或 - n(h)c(= o) - ; R22包括至少一种二价氨基; R 2 3是芳基,取代的芳基,杂芳基,取代的杂芳基,环烷基,取代的环烷基,杂环烷基,取代的杂环烷基,烷氧基,芳氧基,含硫氧脲基团或含Seleno的基团; A,B,C和D独立为0或1。

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