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@misc{838523,
author = {Guzi, Timothy and Paruch, Kamil and Mallams, Alan and Rivera, Jocelyn and Doll, Ronald and Girijavallabhan, Viyyoor and Pachter, Jonathan and Liu, YiandTsung and Saksena, Anil},
keywords = {hydroxysteroid dehydrogenase; inhibitor; prostate cancer},
language = {eng},
title = {17beta Hydroxysteroid Dehydrogenase Type 3 Inhibitors for the Treatment of Androgen Dependent Diseases},
year = {2003}
}
TY - PAT
ID - 838523
AU - Guzi, Timothy - Paruch, Kamil - Mallams, Alan - Rivera, Jocelyn - Doll, Ronald - Girijavallabhan, Viyyoor - Pachter, Jonathan - Liu, Yi-Tsung - Saksena, Anil
PY - 2003
TI - 17beta Hydroxysteroid Dehydrogenase Type 3 Inhibitors for the Treatment of Androgen Dependent Diseases
KW - hydroxysteroid dehydrogenase
KW - inhibitor
KW - prostate cancer
N2 - The title compds. [I; R1, R2 = (un)substituted (hetero)aryl, (hetero)arylakyl; R3 = H, OH, alkoxy, alkyl, provided that when X = N, R3 is not OH or alkoxy; R4, R5, R7, R8 = H, OH, alkyl, etc.; R6 = COR15, SO2R15; R9, R10 = H, F, CF3, etc.; R15 = alkyl, cycloalkyl, aryl, etc.; X, Z = C, N] which are useful as inhibitors of Type 3 17.beta.-hydroxysteroid dehydrogenase, were prepd. Thus, treating the amine II.2HCl [X = H] (multi-step synthesis given) with TMSNCO in the presence of TEA in CH2Cl2 afforded 61% II [X = CONH2]. Compds. I have a range of 17.beta.-hydrosteroid dehydrogenase type 3 binding activity from about 0.005 nM to about > 100 nM.
ER -
GUZI, Timothy, Kamil PARUCH, Alan MALLAMS, Jocelyn RIVERA, Ronald DOLL, Viyyoor GIRIJAVALLABHAN, Jonathan PACHTER, Yi-Tsung LIU and Anil SAKSENA. \textit{17beta Hydroxysteroid Dehydrogenase Type 3 Inhibitors for the Treatment of Androgen Dependent Diseases}. 2003.
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