Design, synthesis, and in vivo SAR of a novel series of pyrazolines as potent selective androgen receptor modulators

…, T Sbriscia, O Linton, SG Lundeen, Z Sui

文献索引：Zhang, Xuqing; Li, Xiaojie; Allan, George F.; Sbriscia, Tifanie; Linton, Olivia; Lundeen, Scott G.; Sui, Zhihua Journal of Medicinal Chemistry, 2007 , vol. 50, # 16 p. 3857 - 3869

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被引用次数: 71

摘要

A novel series of pyrazolines 2 have been designed, synthesized, and evaluated by in vivo screening as tissue-selective androgen receptor modulators (SARMs). Structure-activity relationships (SAR) were investigated at the R 1 to R6 positions as well as the core pyrazoline ring and the anilide linker. Overall, strong electron-withdrawing groups at the R1 and R 2 positions and a small group at the R5 and R6 position are optimal for AR agonist ...