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

International Journal of Molecular Sciences

Saleh A. Bahashwan⁵  Ahmed A. Fayed³  Mohamed A. Ramadan²  Abd El-Galil E. Amr¹  Naif O. Al-Harbi⁴ 

[1] National Research Center, Cairo, Dokki 12622, Egypt; E-Mail:;Microbiology and Immunology Departments, College of Medicine, Taibah University, Almadinah Almunawarah 22624, Saudi Arabia; E-Mail:;Respiratory Therapy Department, College of Medical Rehabilitation Sciences, Taibah University, Almadina Almanoara 22624, Saudi Arabia;Pharmacology and Toxicology Department, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia; E-Mail:;Pharmacology and Toxicology Department, College of Pharmacy, Taibah University, Almadinah Almunawarah 22624, Saudi Arabia; E-Mail:

关键词: naphthalinothiazolohydrazine;    pyrazolopyrimidine;    thiazolopyrimidine;    anticancer activities;   

DOI  :  10.3390/ijms151121587

来源: mdpi

【 摘 要 】

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 (LD₅₀)) comparable to Bicalutamide as reference drug. The structures of newly synthesized compounds were confirmed by IR, ¹H-NMR, ¹³C-NMR, and MS spectral data and elemental analysis. The detailed synthesis, spectroscopic data, LD₅₀ values and pharmacological activities of the synthesized compounds are reported.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.