Thiazole‐Based IL‐17 Inhibitors Discovered by Scaffold Morphing
Sign Up to like & getrecommendations! Published in 2024 at "ChemMedChem"
DOI: 10.1002/cmdc.202400851
Abstract: The pro‐inflammatory cytokine interleukin‐17A (IL‐17) plays an important role in the body's defense against bacterial and fungal infections. However, overexpression of IL‐17 has been associated with several diseases, including rheumatoid arthritis, asthma, psoriasis, and even… read more here.
Keywords: based inhibitors; scaffold morphing; discovered scaffold; thiazole based ... See more keywords
Exploration of certain 1,3-oxazole- and 1,3-thiazole-based hydroxamic acids as histone deacetylase inhibitors and antitumor agents.
Sign Up to like & getrecommendations! Published in 2020 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2020.103988
Abstract: Several novel series of hydroxamic acids bearing 2-benzamidooxazole/thiazole (5a-g, 6a-g) or 2-phenylsulfonamidothiazole (8a-c) were designed and synthesized. The compounds were obtained straightforwards via a two step pathway, starting from commercially available ethyl 2-aminooxazole-4-carboxylate or ethyl… read more here.
Keywords: based hydroxamic; inhibitors antitumor; hydroxamic acids; thiazole based ... See more keywords
Synthesis and multicolor, photophysical, thermal, and conductivity properties of poly(imine)s
Sign Up to like & getrecommendations! Published in 2021 at "Journal of The Taiwan Institute of Chemical Engineers"
DOI: 10.1016/j.jtice.2021.05.010
Abstract: Abstract Background Thiazole-based conjugated have been attracted much attention due to their desirable photophysical properties. Based on this, we aimed to prepare thiazole-based poly(imine)s with tunable multicolor emission behavior in the present paper. Methods Thiazole-based… read more here.
Keywords: thiazole based; poly imine; multicolor; behavior ... See more keywords
Tailoring the Physicochemical Properties of Antimicrobial Peptides onto Thiazole-based γ-Peptide Foldamer.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.0c00077
Abstract: Antimicrobial peptides (AMPs) are amphipathic molecules displaying broad-spectrum bactericidal activity providing opportunities to develop new generation of antibiotics. However their use is limited either by poor metabolic stability or high hemolytic activity. We herein addressed… read more here.
Keywords: physicochemical properties; thiazole based; tailoring physicochemical; based peptide ... See more keywords
Design, Synthesis, and In Vitro Anticancer Evaluation of Thiazole-Based Chalcones Linked to Sulfanilamide as Tumor-Associated Carbonic Anhydrase IX and XII Inhibitors.
Sign Up to like & getrecommendations! Published in 2025 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.5c01392
Abstract: Human carbonic anhydrases IX and XII (hCA IX/XII) are overexpressed in various solid tumors and play critical roles in tumor survival and progression, particularly under hypoxic conditions. In this study, a tail-focused design strategy was… read more here.
Keywords: hca xii; anticancer; xii; tumor associated ... See more keywords
Thiazole-Based Tumor Pyruvate Kinase M2 Inhibitors: A Paradigm-Shifting Therapeutic Strategy Targeting Metabolic and Microbial Synergy in Colorectal Cancer.
Sign Up to like & getrecommendations! Published in 2025 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.5c02169
Abstract: Colorectal cancer (CRC) remains a major global health burden, with current treatments primarily focused on eradicating cancer cells. However, chemotherapy-induced gut dysbiosis exacerbates inflammation and disease progression, necessitating innovative therapeutic strategies. While various metabolic inhibitors… read more here.
Keywords: colorectal cancer; cancer; pyruvate kinase; tumor ... See more keywords
Development in the Synthesis of Bioactive Thiazole-Based Heterocyclic Hybrids Utilizing Phenacyl Bromide
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DOI: 10.1021/acsomega.3c10299
Abstract: Heterocyclic hybrid frameworks represent a burgeoning domain within the realms of drug discovery and medicinal chemistry, attracting considerable attention in recent years. Thiazole pharmacophore fragments, inherent in natural products such as peptide alkaloids, metabolites, and… read more here.
Keywords: utilizing phenacyl; phenacyl bromide; thiazole; synthesis ... See more keywords
Design and synthesis of thiazole-based hydroxamate histone deacetylase inhibitors with potent antitumor efficacy by inducing apoptosis, pyroptosis and cell cycle arrest
Sign Up to like & getrecommendations! Published in 2025 at "Scientific Reports"
DOI: 10.1038/s41598-025-08474-5
Abstract: The dysfunction of HDACs is closely related to tumorigenesis and development, which has emerged as an attractive target for cancer therapy. In this study, a series of thiazole-containing hydroxamate derivatives were designed and synthesized as… read more here.
Keywords: thiazole; cell; apoptosis pyroptosis; thiazole based ... See more keywords
Light-induced spin-state switching in Fe(II) spin-crossover complexes with thiazole-based chelating ligands.
Sign Up to like & getrecommendations! Published in 2024 at "Dalton transactions"
DOI: 10.1039/d4dt00308j
Abstract: Homoleptic complexes [Fe(4bt)3](ClO4)2 (1), [Fe(2bt)3](ClO4)2 (2), and [Fe(3tpH)3](ClO4)2 (3) were obtained by a reaction between the Fe(II) precursor salt and the corresponding thiazole-based bidentate ligand (L = 4bt = 4,4'-bithiazole, 2bt = 2,2'-bithiazole, 3tpH =… read more here.
Keywords: spin crossover; state; spin state; thiazole based ... See more keywords
Recent progress in the synthetic and medicinal perspective of imidazo[2,1-b]thiazole derivatives.
Sign Up to like & getrecommendations! Published in 2025 at "Future medicinal chemistry"
DOI: 10.1080/17568919.2025.2552637
Abstract: Imidazo[2,1-b]thiazole represents a privileged heterocyclic moiety in medicinal chemistry which garnered huge attention among the researchers because of its extensive biological properties and ease of synthetic feasibility. Substituted imidazo[2,1-b]thiazole analogs with diverse therapeutic outcomes play… read more here.
Keywords: thiazole based; chemistry; imidazo thiazole; medicinal chemistry ... See more keywords
Synthesis and Biological Evaluation of Thiazole-Based Fibroblast Growth Factor Receptor-1 Inhibitors.
Sign Up to like & getrecommendations! Published in 2022 at "Anti-cancer agents in medicinal chemistry"
DOI: 10.2174/1871520622666220905141248
Abstract: BACKGROUND The Fibroblast Growth Factor Receptor-1 (FGFR-1) is a tyrosine kinase and a validated target for treatment of different cancer types. OBJECTIVE Design and synthesis of novel thiazole-based analogues of anticancer agents. METHODS Series of… read more here.
Keywords: factor receptor; growth factor; thiazole based; fibroblast growth ... See more keywords