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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 recepto...

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Autores principales: Bahashwan, Saleh A., Fayed, Ahmed A., Ramadan, Mohamed A., Amr, Abd El-Galil E., Al-Harbi, Naif O.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2014
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4264242/
https://www.ncbi.nlm.nih.gov/pubmed/25421248
http://dx.doi.org/10.3390/ijms151121587
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author Bahashwan, Saleh A.
Fayed, Ahmed A.
Ramadan, Mohamed A.
Amr, Abd El-Galil E.
Al-Harbi, Naif O.
author_facet Bahashwan, Saleh A.
Fayed, Ahmed A.
Ramadan, Mohamed A.
Amr, Abd El-Galil E.
Al-Harbi, Naif O.
author_sort Bahashwan, Saleh A.
collection PubMed
description 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.
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spelling pubmed-42642422014-12-12 Androgen Receptor Antagonists and Anti-Prostate Cancer Activities of Some Newly Synthesized Substituted Fused Pyrazolo-, Triazolo- and Thiazolo-Pyrimidine Derivatives Bahashwan, Saleh A. Fayed, Ahmed A. Ramadan, Mohamed A. Amr, Abd El-Galil E. Al-Harbi, Naif O. Int J Mol Sci Article 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. MDPI 2014-11-24 /pmc/articles/PMC4264242/ /pubmed/25421248 http://dx.doi.org/10.3390/ijms151121587 Text en © 2014 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Bahashwan, Saleh A.
Fayed, Ahmed A.
Ramadan, Mohamed A.
Amr, Abd El-Galil E.
Al-Harbi, Naif O.
Androgen Receptor Antagonists and Anti-Prostate Cancer Activities of Some Newly Synthesized Substituted Fused Pyrazolo-, Triazolo- and Thiazolo-Pyrimidine Derivatives
title Androgen Receptor Antagonists and Anti-Prostate Cancer Activities of Some Newly Synthesized Substituted Fused Pyrazolo-, Triazolo- and Thiazolo-Pyrimidine Derivatives
title_full Androgen Receptor Antagonists and Anti-Prostate Cancer Activities of Some Newly Synthesized Substituted Fused Pyrazolo-, Triazolo- and Thiazolo-Pyrimidine Derivatives
title_fullStr Androgen Receptor Antagonists and Anti-Prostate Cancer Activities of Some Newly Synthesized Substituted Fused Pyrazolo-, Triazolo- and Thiazolo-Pyrimidine Derivatives
title_full_unstemmed Androgen Receptor Antagonists and Anti-Prostate Cancer Activities of Some Newly Synthesized Substituted Fused Pyrazolo-, Triazolo- and Thiazolo-Pyrimidine Derivatives
title_short Androgen Receptor Antagonists and Anti-Prostate Cancer Activities of Some Newly Synthesized Substituted Fused Pyrazolo-, Triazolo- and Thiazolo-Pyrimidine Derivatives
title_sort androgen receptor antagonists and anti-prostate cancer activities of some newly synthesized substituted fused pyrazolo-, triazolo- and thiazolo-pyrimidine derivatives
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4264242/
https://www.ncbi.nlm.nih.gov/pubmed/25421248
http://dx.doi.org/10.3390/ijms151121587
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