0000000000263886

AUTHOR

Andrew D. Westwell

showing 2 related works from this author

Synthesis of substituted carbamo(dithioperoxo)thioates as potential BCA2-inhibitory anticancer agents

2015

A new, simple, one-step synthetic route to carbamo(dithioperoxo)thioates from commercially available starting materials is described. The key step of this new synthetic approach involves the tetrabromomethane-promoted reaction between secondary amines, carbon disulfide and alkyl thiols under basic conditions at room temperature. New compounds from this series selected for anticancer screening showed selective sub-micromolar activity within BCA2-expressing human breast cancer cell lines.

chemistry.chemical_classificationCarbamo(dithioperoxo)thioateRMCarbon disulfideStereochemistryTetrabromomethaneDrug Discovery3003 Pharmaceutical ScienceOrganic ChemistryTetrabromomethaneCombinatorial chemistryBiochemistrychemistry.chemical_compoundchemistryAnticancer agentDrug DiscoveryBCA2 inhibitorCancer cell linesHuman breastAlkylDisulfiram analogue
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Synthesis and Biological Properties of Benzothiazole, Benzoxazole, and Chromen-4-one Analogues of the Potent Antitumor Agent 2-(3,4-Dimethoxyphenyl)-…

2008

New fluorinated 2-aryl-benzothiazoles, -benzoxazoles, and -chromen-4-ones have been synthesized and their activity against MCF-7 and MDA 468 breast cancer cell lines compared with the potent antitumor benzothiazole 5. Analogues such as 9a, b and 12a, d yielded submicromolar GI50 values in both cell lines; however, none of the new compounds approached 5 in terms of antitumor potency. For 5, binding to the aryl hydrocarbon receptor appeared to be necessary but not sufficient for growth inhibition.

BenzoxazolesBicyclic moleculebiologyStereochemistryCell CycleAntineoplastic AgentsBreast NeoplasmsBenzoxazoleAryl hydrocarbon receptorChemical synthesisIn vitroStructure-Activity Relationshipchemistry.chemical_compoundReceptors Aryl HydrocarbonchemistryBenzothiazoleCell Line TumorDrug Discoverybiology.proteinHumansMolecular MedicineStructure–activity relationshipBenzopyransBenzothiazolesGrowth inhibitionJournal of Medicinal Chemistry
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