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Int. J. Mol. Sci. 2014, 15(11), 21587-21602; doi:10.3390/ijms151121587

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

1
Pharmacology and Toxicology Department, College of Pharmacy, Taibah University, Almadinah Almunawarah 22624, Saudi Arabia
2
Respiratory Therapy Department, College of Medical Rehabilitation Sciences, Taibah University, Almadina Almanoara 22624, Saudi Arabia
3
National Research Center, Cairo, Dokki 12622, Egypt
4
Microbiology and Immunology Departments, College of Medicine, Taibah University, Almadinah Almunawarah 22624, Saudi Arabia
5
Pharmaceutical Chemistry Department, Drug Exploration and Development Chair (DEDC), College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia
6
Pharmacology and Toxicology Department, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia
*
Author to whom correspondence should be addressed.
Received: 6 September 2014 / Revised: 17 November 2014 / Accepted: 18 November 2014 / Published: 24 November 2014
(This article belongs to the Section Biochemistry, Molecular and Cellular Biology)
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Abstract

A series of substituted pyrazole, triazole and thiazole derivatives (213) 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. View Full-Text
Keywords: naphthalinothiazolohydrazine; pyrazolopyrimidine; thiazolopyrimidine; anticancer activities naphthalinothiazolohydrazine; pyrazolopyrimidine; thiazolopyrimidine; anticancer activities
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Bahashwan, S.A.; Fayed, A.A.; Ramadan, M.A.; Amr, A.E.-G.; Al-Harbi, N.O. Androgen Receptor Antagonists and Anti-Prostate Cancer Activities of Some Newly Synthesized Substituted Fused Pyrazolo-, Triazolo- and Thiazolo-Pyrimidine Derivatives. Int. J. Mol. Sci. 2014, 15, 21587-21602.

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