University of Pittsburgh

Zhou Wang

Peter Wipf

Joel Byron Nelson

Erin M Skoda

John S Lazo

James K Johnson

Paul A Johnston

Serene Tai

Keita Takubo

John Milligan

Minh Bao Nguyen

Minh Mindy Bao Nguyen

A compound, or a pharmaceutically acceptable salt or ester thereof, having a formula I of:R—(Z)—(Y)—(R)—X—R—R

Compounds for treating prostate cancer

A compound, or a pharmaceutically acceptable salt or ester thereof, according to formula I:R&#x2014;(Z)&#x2014;(Y)&#x2014;(R)&#x2014;(X)&#x2014;R&#x2014;Rwherein Ris 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(&#x2550;O), &#x2014;S(&#x2550;O)(&#x2550;O)&#x2014;, or NR, wherein Ris H or alkyl; Ris alkanediyl, substituted alkanediyl, cycloalkanediyl, substituted cycloalkanediyl, alkadienyl, substituted alkadienyl, cycloalkenediyl, substituted cycloalkenediyl, alkatrienyl, substituted alkatrienyl; X is &#x2014;C(&#x2550;O)&#x2014;, &#x2014;S(&#x2550;O)(&#x2550;O)&#x2014;, or &#x2014;N(H)C(&#x2550;O)&#x2014;; Rincludes at least one divalent amino radical; Ris 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.

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

A compound, or a pharmaceutically acceptable salt or ester thereof, having a formula I of: R&#x2014;(Z)&#x2014;(Y)&#x2014;(R)&#x2014;X&#x2014;R&#x2014;Rwherein R20 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, halide, or a nitro-containing group; Z is alkanediyl, substituted alkanediyl, cycloalkanediyl, or substituted cycloalkanediyl; Y is S, O, or NR, wherein Ris H or alkyl; Ris alkanediyl, substituted alkanediyl, cycloalkanediyl, substituted cycloalkanediyl, alkadienyl, substituted alkadienyl, alkatrienyl, substituted alkatrienyl; X is &#x2014;C(=0)- or &#x2014;S(=0)(=0)-; Ris a moiety that includes at least one divalent amino radical; Ris an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, halide, or a nitro-containing group; a is 0 or 1; b is 0 or 1; and c is 0 or 1; provided that if X is &#x2014;C(=0)- then Y is not S.

A compound, or a pharmaceutically acceptable salt or ester thereof, according to formula I:R&#x2014;(Z)&#x2014;(Y)&#x2014;(R)&#x2014;(X)&#x2014;R&#x2014;Rwherein Ris 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(&#x2550;O), &#x2014;S(&#x2550;O)(&#x2550;O)&#x2014;, or NR, wherein Ris H or alkyl; Ris alkanediyl, substituted alkanediyl, cycloalkanediyl, substituted cycloalkanediyl alkadienyl, substituted alkadienyl, alkatrienyl, substituted alkatrienyl; X is &#x2014;C(&#x2550;O)&#x2014;, &#x2014;S(&#x2550;O)(&#x2550;O)&#x2014;, or &#x2014;N(H)C(&#x2550;O)&#x2014;; Rincludes at least one divalent amino radical; Ris 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.

A method for treating prostate cancer in a subject, comprising administering a therapeutically effective amount of at least one agent to the subject, wherein the agent is selected from: 

Small molecules targeting androgen receptor nuclear localization and/or level in prostate cancer

A method for treating prostate cancer in a subject, comprising administering a therapeutically effective amount of at least one agent to the subject, wherein the agent is selected from: wherein Ris an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, halide, or a nitro-containing group;

Growing community of inventors

Pittsburgh, PA, United States of America

Zhou Wang