Synthesis, biological evaluation, and molecular modeling of abiraterone analogues: novel CYP17 inhibitors for the treatment of prostate cancer

MAE Pinto-Bazurco Mendieta, M Negri…

Index: Pinto-Bazurco Mendieta, Mariano A.E.; Negri, Matthias; Jagusch, Carsten; Hille, Ulrike E.; Mueller-Vieira, Ursula; Schmidt, Dirk; Hansen, Klaus; Hartmann, Rolf W. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 1 p. 267 - 273

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Citation Number: 39

Abstract

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 effects attributable to their structure, we have tried to replace the sterane scaffold by nonsteroidal core structures. The design and synthesis of 20 new abiraterone mimetics are described. ...