A novel series of pyrazolines I 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 R1, R2, R3 and R4 on the left-side aromatic ring, R5 at the angular carbon, R6 on the pyrazole ring, as well as the core pyrazoline ring and the anilide linker. The lead compound was identified as a tissue-selective androgen receptor modulator. The androgenic, anabolic and antiandrogenic activity of the lead compound was evaluated in both castrated and intact mature male rat models. It exhibited an overall partial androgenic effect, but full anabolic effect via oral administration in castrated rats. The lead compound further demonstrated a noticeable antiandrogenic effect on prostate in intact rats supplemented with testosterone propionate. Thus, it is a tissue-selective non-steroidal androgen receptor modulator with agonist activity on muscle and mixed agonist and antagonist activity on prostate, which can be used for the treatment of male hypogonadism, muscle wasting and osteoporosis and female sexual dysfunction.