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




Androgen Receptor Antagonists and Anti-Prostate Cancer Activities of Some Newly Synthesized Substituted Fused Pyrazolo-, Triazolo- and Thiazolo-Pyrimidine Derivatives - Download this document for free, or read online. Document in PDF available to download.

1

Pharmacology and Toxicology Department, College of Pharmacy, Taibah University, Almadinah Almunawarah 22624, Saudi Arabia

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Respiratory Therapy Department, College of Medical Rehabilitation Sciences, Taibah University, Almadina Almanoara 22624, Saudi Arabia

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National Research Center, Cairo, Dokki 12622, Egypt

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Microbiology and Immunology Departments, College of Medicine, Taibah University, Almadinah Almunawarah 22624, Saudi Arabia

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Pharmaceutical Chemistry Department, Drug Exploration and Development Chair DEDC, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia

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Pharmacology and Toxicology Department, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia





*

Author to whom correspondence should be addressed.



Abstract A series of substituted pyrazole, triazole and thiazole derivatives 2–13 were synthesized from 1-naphtho1,2-dthiazol-2-ylhydrazine 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





Author: Saleh A. Bahashwan 1, Ahmed A. Fayed 2,3,* , Mohamed A. Ramadan 4, Abd El-Galil E. Amr 3,5 and Naif O. Al-Harbi 6

Source: http://mdpi.com/



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