4-(Anilino) pyrrole-2-carboxamides: Novel non-steroidal/non-anilide type androgen antagonists effective upon human prostate tumor LNCaP cells with mutated …

K Wakabayashi, K Imai, H Miyachi, Y Hashimoto…

Index: Wakabayashi, Ken-ichi; Imai, Keisuke; Miyachi, Hiroyuki; Hashimoto, Yuichi; Tanatani, Aya Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 14 p. 6799 - 6812

Full Text: HTML

Citation Number: 11

Abstract

Various 4-(anilino) pyrrole-2-carboxamides were designed and synthesized as novel androgen receptor (AR) antagonists without steroidal or anilide structure, based on our strategy for developing full antagonists of nuclear receptors. Introduction of a bulky N-alkyl group, such as a cyclohexylmethyl or benzyl group, increased the binding affinity for wild- type AR and the potency for growth inhibition of androgen-dependent SC-3 cells. Among ...