Discovery of tropinone-thiazole derivatives as potent caspase 3/7 activators, and noncompetitive tyrosinase inhibitors with high antiproliferative activity: Rational design, one-pot tricomponent synthesis, and lipophilicity determination.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.05.006
Abstract: We have designed novel tropinone-thiazole derivatives that showed high antiproliferative activity against a variety of cancer cell lines via caspase 3/7 activation mechanism. Among the derivatives, compounds 3b-3h were found to exhibit high activity against… read more here.
Keywords: activity; tropinone thiazole; thiazole derivatives; antiproliferative activity ... See more keywords
A novel access to 4-trifluoromethyl-1,3-thiazole derivatives via an intermediate thiocarbonyl ylide
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Fluorine Chemistry"
DOI: 10.1016/j.jfluchem.2019.02.003
Abstract: Abstract A Lewis acid catalyzed reaction of trifluoroacetyldiazomethane (CF3COCHN2) with thiourea occurs in boiling THF solution in the presence of BF3·OEt2 yielding 2-amino-4-trifluoromethyl-1,3-thiazole in a fair yield. Analogous reactions with aromatic thioamides, performed in the… read more here.
Keywords: trifluoromethyl thiazole; thiazole derivatives; access trifluoromethyl; derivatives via ... See more keywords
Synthesis and Molecular Docking Study of New Thiazole Derivatives as Potential Tubulin Polymerization Inhibitors
Sign Up to like & getrecommendations! Published in 2022 at "ACS Omega"
DOI: 10.1021/acsomega.2c05077
Abstract: A new series of 2,4-disubstituted thiazole derivatives containing 4-(3,4,5-trimethoxyphenyl) moiety was synthesized and evaluated for their potential anticancer activity as tubulin polymerization inhibitors. All designed compounds were screened for cytotoxic activity against four human cancer… read more here.
Keywords: molecular docking; polymerization inhibitors; thiazole derivatives; activity ... See more keywords
Design, synthesis and docking studies of novel thiazole derivatives incorporating pyridine moiety and assessment as antimicrobial agents
Sign Up to like & getrecommendations! Published in 2021 at "Scientific Reports"
DOI: 10.1038/s41598-021-86424-7
Abstract: A novel series of substituted 4,6-dimethyl-2-oxo-1-(thiazol-2-ylamino)-1,2-dihydropyridine-3-carbonitrile derivatives 6, 9, 13, 15, and 17 was synthesized in a good to excellent yield from the reaction of 1-(3-cyano-4,6-dimethyl-2-oxopyridin-1(2H)-yl)thiourea with 2-oxo-N'-arylpropanehydrazonoyl chloride, chloroacetone, α-bromoketones, ethyl chloroacetate, and 2,3-dichloroquinoxaline,… read more here.
Keywords: design synthesis; studies novel; synthesis docking; docking studies ... See more keywords
Modular synthesis of thiazoline and thiazole derivatives by using a cascade protocol
Sign Up to like & getrecommendations! Published in 2017 at "Rsc Advances"
DOI: 10.1039/c7ra05993k
Abstract: The first common synthetic protocol for thiazolines and thiazoles. read more here.
Keywords: modular synthesis; protocol; synthesis thiazoline; thiazoline thiazole ... See more keywords
Novel 2-(2-hydrazinyl)thiazole derivatives as chemotherapeutic agents
Sign Up to like & getrecommendations! Published in 2020 at "Synthetic Communications"
DOI: 10.1080/00397911.2020.1791344
Abstract: Abstract A series of 2-(2-hydrazinyl)thiazole derivatives containing diarylsulfide moiety were synthesized and investigated for their antibacterial and antifungal activities. Compound 3j, namely 2-[2-[4-((4-fluorophenyl)thio)benzylidene]hydrazinyl]-4-(4-methylphenyl)thiazole was determined as the most potent antifungal agent. It was further tested… read more here.
Keywords: novel hydrazinyl; chemotherapeutic agents; hydrazinyl thiazole; derivatives chemotherapeutic ... See more keywords
Anti-viral activity of thiazole derivatives: an updated patent review.
Sign Up to like & getrecommendations! Published in 2022 at "Expert opinion on therapeutic patents"
DOI: 10.1080/13543776.2022.2067477
Abstract: INTRODUCTION : Several viral infections cause life-threatening consequences in humans, making them the most serious worldwide public health concerns. Despite the fact that several antiviral medicines are available on the market, there is no full… read more here.
Keywords: review; thiazole derivatives; viral infections; activity ... See more keywords
Design, synthesis and cytotoxic evaluation of novel bis-thiazole derivatives as preferential Pim1 kinase inhibitors with in vivo and in silico study
Sign Up to like & getrecommendations! Published in 2023 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2023.2166936
Abstract: Abstract Bis-thiazole derivatives were synthesised conforming to the Pim1 pharmacophore model following Hantzsch condensation. Pim1 has a major role in regulating the G1/S phase which upon inhibition the cell cycle stops at its early stages.… read more here.
Keywords: thiazole derivatives; bis thiazole; pim1; cytotoxic evaluation ... See more keywords
One-pot PEG-mediated syntheses of 2-(2-hydrazinyl) thiazole derivatives: novel route
Sign Up to like & getrecommendations! Published in 2018 at "Journal of Sulfur Chemistry"
DOI: 10.1080/17415993.2017.1371175
Abstract: ABSTRACT Thiazoles are important sulfur-containing molecules that are widely used in diverse fields such as pharmaceuticals, agrochemicals, and material sciences. This is the first report on the PEG-300-mediated one-pot synthesis of 2-(2-hydrazinyl) thiazole derivatives from… read more here.
Keywords: pot peg; peg 300; hydrazinyl thiazole; thiazole derivatives ... See more keywords
Tackling Microbial Resistance with Isatin-Decorated Thiazole Derivatives: Design, Synthesis, and in vitro Evaluation of Antimicrobial and Antibiofilm Activity
Sign Up to like & getrecommendations! Published in 2022 at "Drug Design, Development and Therapy"
DOI: 10.2147/dddt.s365909
Abstract: Introduction Antibiotic resistance is a global threat that has been increasing recently, especially with antibiotic overuse and misuse. The search for new antibiotics is becoming more and more indispensable. Methods Design and synthesis of isatin… read more here.
Keywords: design synthesis; antimicrobial antibiofilm; decorated thiazole; thiazole derivatives ... See more keywords
Synthesis and Evaluation of A New Series of Thiazole Derivatives as Potential Antitumor Agents and MMP Inhibitors.
Sign Up to like & getrecommendations! Published in 2017 at "Anti-cancer agents in medicinal chemistry"
DOI: 10.2174/1871520616666160802113620
Abstract: BACKGROUND In recent years, the relationship between overexpression of matrix metalloproteinases (MMPs) and tumor invasion/metastasis has prompted researchers to develop MMP inhibitors as anticancer drugs. OBJECTIVE The aim of this study was to design and… read more here.
Keywords: mcf; mmp inhibitors; mmp; thiazole derivatives ... See more keywords