New 3‐Substituted‐2‐(4‐hydroxyanilino)pyridine Derivatives: Synthesis, Antitumor Activity, and Tubulin Polymerization Inhibition
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DOI: 10.1002/ardp.201600256
Abstract: A series of new pyridine derivatives 4a–c, 5a–d, 6a–d, 7a–f, and 8a–f structurally related to ABT‐751 were synthesized and characterized by spectroscopic means and elemental analysis. All the synthesized compounds were tested for their cytotoxic… read more here.
Keywords: new substituted; inhibition; substituted hydroxyanilino; tubulin ... See more keywords
Design, synthesis, and biological evaluation of novel 3‐(thiophen‐2‐ylthio)pyridine derivatives as potential multitarget anticancer agents
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DOI: 10.1002/ardp.201900024
Abstract: A series of novel 3‐(thiophen‐2‐ylthio)pyridine derivatives as insulin‐like growth factor 1 receptor (IGF‐1R) inhibitors was designed and synthesized. IGF‐1R kinase inhibitory activities and cytotoxicities against HepG2 and WSU‐DLCL2 cell lines were tested. For all of… read more here.
Keywords: ylthio pyridine; novel thiophen; anticancer agents; multitarget anticancer ... See more keywords
Synthesis and evaluation of anticonvulsant activities of 7‐phenyl‐4,5,6,7‐tetrahydrothieno[3,2‐b ]pyridine derivatives
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DOI: 10.1002/ardp.201900106
Abstract: A series of 7‐phenyl‐4,5,6,7‐tetrahydrothieno[3,2‐b]pyridine derivatives containing triazole and other heterocycle substituents (methyltriazole, tetrazole, and triazolone) is described. Two experimental methods, maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ), were used to evaluate the anticonvulsant activity of… read more here.
Keywords: pyridine; tetrahydrothieno pyridine; evaluation anticonvulsant; synthesis evaluation ... See more keywords
Novel pyrazolo[3,4‐b]pyridine derivatives: Synthesis, structure–activity relationship studies, and regulation of the AMPK/70S6K pathway
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DOI: 10.1002/ardp.202100465
Abstract: A series of novel pyrazolo[3,4‐b]pyridine derivatives were designed, synthesized, and biologically evaluated for anti‐lung cancer activity. Structure–activity relationship and AutoGPA models were constructed based on the in vitro antiproliferative potency of the compounds against a… read more here.
Keywords: novel pyrazolo; structure activity; pyrazolo pyridine; pyridine derivatives ... See more keywords
Imidazo[1,2‐a]pyridine Derivatives as AMPK Activators: Synthesis, Structure–Activity Relationships, and Regulation of Reactive Oxygen Species in Renal Fibroblasts
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DOI: 10.1002/cmdc.202200696
Abstract: Adenosine 5′‐monophosphate activated protein kinase (AMPK) has emerged as a promising target for the discovery of drugs to treat diabetic nephropathy (DN). Herein, a series of imidazo[1,2‐a]pyridines were designed and synthesized. Among them, the active… read more here.
Keywords: reactive oxygen; imidazo pyridine; oxygen species; pyridine derivatives ... See more keywords
Silver‐Catalyzed Synthesis of Substituted Pyridine Derivatives from N‐Propargylic α‐Enamino Esters
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DOI: 10.1002/ejoc.201700559
Abstract: A wide range of substituted pyridine derivatives were synthesized in moderate to good yields from a N-propargylic α-enamino ester. The synthetic strategy involves regioselective addition of propargyl amine to the α-carbon of the alkynyl ester… read more here.
Keywords: substituted pyridine; synthesis; propargylic enamino; pyridine derivatives ... See more keywords
Design, cytotoxicity and toxicity of new thiophene and thieno [2,3-b] pyridine derivatives
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DOI: 10.1007/s00044-017-1780-6
Abstract: Novel thiophene derivatives 3a–f were synthesized by using the 3-oxo-3-propanenitrile derivatives 1a–c with triethylamine, elemental sulfur and either of malononitrile or ethyl cyanoacetate. Compounds 3a, 3c, and 3e were reacted with ethyl cyanoacetate to give… read more here.
Keywords: thiophene; design cytotoxicity; cancer; thieno pyridine ... See more keywords
Synthesis of 2-(1-aryl-1H-tetrazol-5-yl)-thieno[2,3-b]pyridine derivatives
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DOI: 10.1007/s10593-019-02533-2
Abstract: Alkylation of 4,6-dimethyl-2-sulfanylpyridine-3-carbonitrile with 1-aryl-5-(chloromethyl)-1H-tetrazoles yielded 2-{[(1-aryl-1H-tetrazol-5-yl)methyl]sulfanyl}-4,6-dimethylpyridine-3-carbonitriles, which easily cyclize by the action of bases to form 2-(1H-tetrazol-5-yl)-thieno[2,3-b]pyridine derivatives. The use of excess base in the alkylation step leads to direct formation of cyclized products… read more here.
Keywords: aryl tetrazol; thieno pyridine; tetrazol thieno; pyridine derivatives ... See more keywords
Reusable photoresponsive Ag/AgCl nanocube-catalyzed one-pot synthesis of seleno[2,3-b]pyridine derivatives
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DOI: 10.1007/s11164-020-04143-6
Abstract: In this study, a facile and rapid method was developed to synthesize intensely organoselenium compounds, namely ethylseleno[2,3-b]pyridine carboxylate, seleno[2,3-b]pyridine-2-carbonitrile and 2-benzoylseleno[2,3-b]pyridine derivatives from starting compound, 2-chloro-3-cyano-4,6-dimethylpyridine, in one-pot synthesis using Ag/AgCl nanoparticles (NPs) under visible… read more here.
Keywords: seleno pyridine; pot synthesis; one pot; agcl ... See more keywords
Discovery of novel 2-substituted-4-(2-fluorophenoxy) pyridine derivatives possessing pyrazolone and triazole moieties as dual c-Met/VEGFR-2 receptor tyrosine kinase inhibitors.
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DOI: 10.1016/j.bioorg.2017.04.001
Abstract: In our efforts to develop novel dual c-Met/VEGFR-2 inhibitors as potential anticancer agents, a series of 2-substituted-4-(2-fluorophenoxy) pyridine derivatives bearing pyrazolone scaffold were designed and synthesized. The cell proliferation assay in vitro demonstrated that most… read more here.
Keywords: substituted fluorophenoxy; met vegfr; fluorophenoxy pyridine; dual met ... See more keywords
Design, synthesis and biological evaluation of pyridine derivatives as selective SHP2 inhibitors.
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DOI: 10.1016/j.bioorg.2020.103875
Abstract: SHP2 is a non-receptor protein tyrosine phosphatase encoded by the PTPN11 gene, which affects the transduction of multiple signaling pathways, including RAS-ERK, PI3K-AKT and JAK-STAT. SHP2 also plays an important role in the programmed cell… read more here.
Keywords: selective shp2; shp2; shp2 inhibitors; activity ... See more keywords