Synthesis and structure-activity relationships of thieno[2,3-d]pyrimidine-2,4-dione derivatives as potent GnRH receptor antagonists.

doi:10.1016/S0960-894X(03)00746-7

Paper

DOI: 10.1016/S0960-894X(03)00746-7

Synthesis and structure-activity relationships of thieno[2,3-d]pyrimidine-2,4-dione derivatives as potent GnRH receptor antagonists.

Published Oct 20, 2003 · Zhiqian Guo, Yongsheng Chen, Dongpei Wu

Bioorganic & medicinal chemistry letters

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Abstract

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In Vitro Study

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Thieno[2,3-d]pyrimidine-2,4-dione derivatives show potential as potent human GnRH receptor antagonists for treating reproductive diseases, with a binding affinity of 0.4 nM.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Discovery of a thieno[2,3-d]pyrimidine-2,4-dione bearing a p-methoxyureidophenyl moiety at the 6-position: a highly potent and orally bioavailable non-peptide antagonist for the human luteinizing hormone-releasing hormone receptor.

Compound 9k, a thieno[2,3-d]pyrimidine-2,4-dione derivative with a biaryl moiety, is a highly potent and orally bioavailable non-peptide LHRH antagonist with potential applications in hormone replacement therapy.

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Synthesis and initial structure-activity relationships of a novel series of imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists.

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Design, synthesis and structure-activity relationships of novel imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists.

Compound 10b, a novel imidazolo[1,2-a]pyrimid-5-one, shows higher potency as a GnRH receptor antagonist than previous compounds 2a and 2b, with a methyl group at the 7-position and 3-methoxyphenyl group at the 6-

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The best compound from the series, 2-(2-Methylaminoethyl)pyridine, shows 25 nM binding affinity to human GnRH receptor, making it a promising GnRH receptor antagonist.

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RP-010 shows potential as an efficacious and relatively nontoxic anticancer compound for prostate cancer, inducing -catenin fragmentation and causing mitotic catastrophe and apoptosis in prostate cancer cells.

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The Novel Thienopyrimidine Derivative, RP-010, Produces Its Efficacy in Prostate Cancer Cells by Inducing the Fragmentation of β-catenin

RP-010 shows promising anticancer activity in metastatic prostate cancer cells by inducing -catenin fragmentation and decreased migration and invasiveness without significant toxicity in zebrafish.

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Design, Synthesis and Biological Evaluation of Some 5-Arylthieno[2,3-d]pyrimidines as Potential Anti-cancer Agents.

Two potent lead compounds, 3b and f, show excellent cytotoxic activity and enzymatic inhibition activity against MCF-7 cancer cells.

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A facile synthesis of some novel fused [1,2,4]triazolo[3,4-b][1,3,4]thiadiazol derivatives

This study presents a facile method for synthesizing novel fused [1,2,4]triazolo[3,4-b][1,3,4]thiadiazol derivatives, offering potential applications in pharmaceuticals and nutraceuticals.

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Discovery of 1-{4-[1-(2,6-difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a potent, orally active, non-peptide antagonist of the human gonadotropin-releasing hormone receptor.

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Novel Thiophenes, Thienopyrimidines, and Triazolothienopyrimidines for the Evaluation of Anticancer and Augmentation Effects of γ‐Radiation

Novel thiophenes, thienopyrimidines, and triazolothienopyrimidines show significant in-vitro anticancer activity, with compounds 2, 3, 10, 11, and 12 showing the most potent in-vitro anticancer activity when combined with radiation

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