289056-04-8Relevant articles and documents
Synthesis, biological evaluation, and molecular modeling of abiraterone analogues: Novel CYP17 inhibitors for the treatment of prostate cancer
Pinto-Bazurco Mendieta, Mariano A. E.,Negri, Matthias,Jagusch, Carsten,Müller-Vieira, Ursula,Lauterbach, Thomas,Hartmann, Rolf W.
supporting information; experimental part, p. 5009 - 5018 (2009/07/04)
Abiraterone, a steroidal cytochrome P450 17α-hydroxylase-17,20-lyase inhibitor (CYP17), is currently undergoing phase II clinical trials as a potential drug for the treatment of androgen-dependent prostate cancer. Since steroidal compounds often show side
Novel imidazolyl and triazolyl substituted biphenyl compounds: Synthesis and evaluation as nonsteroidal inhibitors of human 17α-Hydroxylase-C17, 20-lyase (P450 17)
Zhuang, Yan,Wachall, Bertil G.,Hartmann, Rolf W.
, p. 1245 - 1252 (2007/10/03)
The synthesis of a new series of P450 17 inhibitors is described. The imidazol-1-yl compounds 5 showed strong inhibition of P450 17 rat and especially human enzyme, the most active compounds being 5ax, 5ay and 5bx with IC50 values of 0.17, 0.24 and 0.25 μM, respectively (ketoconazole: 0.74 μM). The 1,2,4-triazol-1-yl compounds 6 were less active, while the 1,2,4-triazol-4-yl compounds 7 were inactive. The title compounds showed little inhibition of P450 arom. The most active P450 17 inhibitors 5ax and 5ay markedly decreased the testosterone plasma concentration of SD rats 2 h after application of 0.019 mmol/kg. After 6 h, 5ay still exhibited a strong effect. Copyright (C) 2000 Elsevier Science Ltd.