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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...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2014
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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. |
format | Online Article Text |
id | pubmed-4264242 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2014 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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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