Synthesis and antiandrogenic activity of some new 3-substituted androstano[17,16-c]-5'-aryl-pyrazoline and their derivatives.
A series of androstano[17,16-c]pyrazolines and their oxidized derivatives (2-14) were synthesized using 3beta-hydroxyandrostan-17-one as a starting material (1a, b). The synthesized compounds were evaluated for their antiandrogenic activity compared to that of Cyproterone as positive control. Some of the compounds exhibited better antiandrogenic activity than the reference drug. The detailed synthesis, spectroscopic data, ED(50), and toxicity (LD(50) and LD(90)) of the synthesized compounds were reported.
Amr
Abd El-Galil E
Ael-G
Applied Organic Chemistry Department, National Research Centre, Dokki, Cairo, Egypt. aamr1963@yahoo.com
Abdel-Latif
Nehad A
NA
Abdalla
Mohamed M
MM
D000726:Androgen Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D000818:Animals; D005260:Female; D007928:Lethal Dose 50; D009682:Magnetic Resonance Spectroscopy; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D051381:Rats; D017207:Rats, Sprague-Dawley; D021241:Spectrometry, Mass, Electrospray Ionization; D013055:Spectrophotometry, Infrared
D000726:Androgen Antagonists; D011720:Pyrazoles