Androgen Receptor Antagonists and Anti-Prostate Cancer Activities of Some Newly Synthesized Substituted Fused Pyrazolo-, Triazolo- and Thiazolo-Pyrimidine Derivatives

A series of substituted pyrazole, triazole and thiazole derivatives (2–13) were synthesized from 1-(naphtho[1,2-d]thiazol-2-yl)hydrazine as starting material and evaluated as androgen receptor antagonists and anti-prostate cancer agents. The newly synthesized compounds showed potent androgen receptor antagonists and anti-prostate cancer activities with low toxicity (lethal dose 50 (LD(50))) comparable to Bicalutamide as reference drug. The structures of newly synthesized compounds were confirmed by IR, (1)H-NMR, (13)C-NMR, and MS spectral data and elemental analysis. The detailed synthesis, spectroscopic data, LD(50) values and pharmacological activities of the synthesized compounds are reported.