Journal ArticleDOI
Identification of oxazolidinediones and thiazolidinediones as potent 17β-hydroxysteroid dehydrogenase type 3 inhibitors.
TLDR
5-(3-Bromo-4-hydroxybenzylidene)-3-(4-methoxyphenyl)-2-thioxo-1,3-thiazolidin- 4-one exhibited a promising activity profile and demonstrated significant selectivity over the related 17β-HSD isoenzymes and nuclear receptors.About:
This article is published in Bioorganic & Medicinal Chemistry Letters.The article was published on 2012-01-01. It has received 19 citations till now. The article focuses on the topics: Oxazolidinedione & Hydroxysteroid dehydrogenase.read more
Citations
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Rhodanine as a scaffold in drug discovery: a critical review of its biological activities and mechanisms of target modulation.
TL;DR: The biological activity of compounds possessing a rhodanine moiety should be considered very critically despite the convincing data obtained in biological assays.
Journal ArticleDOI
Recent Advances in the Synthesis of Hydantoins: The State of the Art of a Valuable Scaffold
TL;DR: Novel synthetic routes to various hydantoin structures, the advances brought to the classical methods in the aim of producing more sustainable and environmentally friendly procedures for the preparation of these biomolecules, and a critical comparison of the different synthetic approaches developed in the last twelve years are described.
Journal ArticleDOI
Multicomponent reactions: a sustainable tool to 1,2- and 1,3-azoles.
Preeti,Krishna Nand Singh +1 more
TL;DR: This critical review covers the journey of MCRs to 1,2/1,3-azoles including the synthetic strategies, scope, reaction conditions, rationale behind the choice of catalyst and the proposed mechanism.
Journal ArticleDOI
Chemical fixation of carbon dioxide by copper catalyzed multicomponent reactions for oxazolidinedione syntheses
TL;DR: It is demonstrated that the fixation of CO2 for oxazolidinedione synthesis via a novel multicomponent synthesis in the presence of a catalytic amount of Cu2O, various 2-bromo-3-phenylacrylic acid derivatives reacted with CO2 and amines are transformed to the corresponding oxazolicinedione derivatives in high yields.
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Intratumoral steroidogenesis in castration-resistant prostate cancer: a target for therapy.
Inna Armandari,Agus Rizal Ardy Hariandy Hamid,Agus Rizal Ardy Hariandy Hamid,Gerald W. Verhaegh,Jack A. Schalken +4 more
TL;DR: Several studies now have demonstrated that PCa cells are able to produce T and DHT from different androgen precursors, such as cholesterol and the adrenal androgen, dehydroepiandrosterone (DHEA).
References
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Journal ArticleDOI
Molecular characterization of human prostate carcinoma cell lines
Adrie van Bokhoven,Marileila Varella-Garcia,Christopher Korch,Widya U. Johannes,E. Erin Smith,Heidi L. Miller,Steven K. Nordeen,Gary J. Miller,M. Scott Lucia +8 more
TL;DR: This study presents a comprehensive survey and characterization of available prostate carcinoma cell lines, most of which have been widely used but are incompletely characterized.
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Inhibitors of 17 beta-hydroxysteroid dehydrogenases.
TL;DR: In addition to giving an up-to-date description of inhibitors of all 17beta-HSD isoforms (types 1-8), the present review will also address, when possible, the isoform selectivity and residual estrogenic or androgenic activity often associated with steroidal inhibitors.
Journal ArticleDOI
A guide to 17β-hydroxysteroid dehydrogenases
Jerzy Adamski,Franz Jakob +1 more
TL;DR: A review of 17β-hydroxysteroid dehydrogenases (17β-HSD) can be found in this article, which summarizes recent progress in the field and provides an update of nomenclature.
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Design, synthesis, and biological evaluation of N-carboxyphenylpyrrole derivatives as potent HIV fusion inhibitors targeting gp41.
Kun Liu,Hong Lu,Ling Hou,Zhi Qi,Cátia Teixeira,Florent Barbault,Botao Fan,Shuwen Liu,Shibo Jiang,Lan Xie +9 more
TL;DR: The most active compound, N-(3-carboxy-4-hydroxy)phenyl-2,5-dimethylpyrrole (A(12), partially occupied the deep hydrophobic pocket, suggesting that enlarging the molecular size of A(12) could improve its binding affinity and anti-HIV-1 activity for further development as a small-molecule HIV fusion and entry inhibitor.
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Differential expression of 17β‐hydroxysteroid dehydrogenase isozyme genes in prostate cancer and noncancer tissues
TL;DR: This study presents the differential expression of 17βHSD isozyme genes in cancerous and noncancerous prostate tissues of in vivo samples.