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Bioorg Chem ; 81: 468-480, 2018 12.
Artigo em Inglês | MEDLINE | ID: mdl-30243238

RESUMO

In the present study, novel 2-cyclopropyl-3-ethynyl-4-(4-fluorophenyl) quinolines (4a-l) were recognized and evaluated as G-Protein Coupled Receptor (GPCR) ligands through molecular evaluations. Thrombin mediates adhesion of mast cell, a type of cell abundantly found in connective tissue and releasing histamine and other substances during inflammatory and allergic reactions, through phosphoinositol 3-kinase pathway. With this background, as preliminary, 4a-l are resolute to be potential leads, designated from their effective phosphoinositol 3-kinase (PI3-Kinase) inhibition potentials, best-docked scores, comparative ligand efficiency, and significant structural attributes evaluated by ab initio simulations. Since thrombin is one of the main reason for various cancer invasion in association with PI3Kinase, a thrombolytic potential of the compounds also analyzed. The experimental in vitro studies confirmed the significant enhancement as PI3Kinase inhibitors and appreciable enhancement in MTT assay of breast and skin cancer cell lines. Significantly, acetophenone substituent in the quinoline scaffold could be coherent to note the significant binding affinity to all the evaluated drug targets.


Assuntos
Antineoplásicos/farmacologia , Fibrinolíticos/farmacologia , Inibidores de Fosfoinositídeo-3 Quinase , Agregação Plaquetária/efeitos dos fármacos , Quinolinas/farmacologia , Receptor PAR-1/antagonistas & inibidores , Antineoplásicos/química , Linhagem Celular Tumoral , Descoberta de Drogas , Fibrinolíticos/química , Halogenação , Humanos , Ligantes , Simulação de Acoplamento Molecular , Neoplasias/tratamento farmacológico , Neoplasias/metabolismo , Fosfatidilinositol 3-Quinases/metabolismo , Quinolinas/química , Receptor PAR-1/metabolismo , Receptores Acoplados a Proteínas G/metabolismo
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