beta-Alkylthio indolyl carbinols: potent nonsteroidal antiandrogens with oral efficacy in a prostate cancer model.
Through an in vivo screening model, we developed the in vivo SAR of beta-alkylthio indolyl carbinols. Through these efforts we identified a compound with potent oral in vivo efficacy in both immature and mature rat prostate weight reduction models and in a murine xenograft prostate cancer model.
Lanter
James C
JC
Johnson & Johnson Pharmaceutical Research and Development L.L.C., 665 Stockton Drive, Exton, PA 19341, USA. jlanter@prdus.jnj.com
Fiordeliso
James J
JJ
Alford
Vernon C
VC
Zhang
Xuqing
X
Wells
Kenneth M
KM
Russell
Ronald K
RK
Allan
George F
GF
Lai
Muh-Tsann
MT
Linton
Olivia
O
Lundeen
Scott
S
Sui
Zhihua
Z
D000284:Administration, Oral; D000726:Androgen Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000138:chemical synthesis*; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D004195:Disease Models, Animal; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology; D008297:Male; D000432:Methanol / Q000031:analogs & derivatives* / Q000737:chemistry*; D051379:Mice; D009368:Neoplasm Transplantation; D011471:Prostatic Neoplasms / Q000188:drug therapy*; D051381:Rats; D013329:Structure-Activity Relationship
D000726:Androgen Antagonists; D000970:Antineoplastic Agents; D007211:Indoles; D000432:Methanol