Pimentel, Luiz Claudio Ferreira; Hoelz, Lucas Villas Boas; Canzian, Henayle Fernandes; Branco, Frederico Silva Castelo; Paula de Oliveira, Andressa; Campos, Vinicius Rangel; Silva, Floriano Paes Jr.; Dantas, Rafael Ferreira; Resende, Jackson Antonio Lamounier Camargos; Cunha, Anna Claudia; Boechat, Nubia; Bastos, Monica Macedo published their research in Beilstein Journal of Organic Chemistry in 2021. The article was titled 《The (Phenylamino)pyrimidine-1,2,3-triazole derivatives as analogs of imatinib: searching for novel compounds against chronic myeloid leukemia》.Recommanded Product: Ethyl propiolate The article contains the following contents:
The enzyme tyrosine kinase BCR-Abl-1 is the main mol. target in the treatment of chronic myeloid leukemia and can be competitively inhibited by tyrosine kinase inhibitors such as imatinib. New potential competitive inhibitors were synthesized using the (phenylamino)pyrimidine-pyridine (PAPP) group as a pharmacophoric fragment, and these compounds were biol. evaluated. The synthesis of twelve new compounds was performed in three steps and assisted by microwave irradiation in a 1,3-dipolar cycloaddition to obtain 1,2,3-triazole derivatives substituted on carbon C-4 of the triazole nucleus. All compounds were evaluated for their inhibitory activities against a chronic myeloid leukemia cell line (K562) that expresses the enzyme tyrosine kinase BCR-Abl-1 and against healthy cells (WSS-1) to observe their selectivity. Three compounds showed promising results, with IC50 values between 1.0 and 7.3 μM, and were subjected to mol. docking studies. The results suggest that such compounds can interact at the same binding site as imatinib, probably sharing a competitive inhibition mechanism. One compound showed the greatest interaction affinity for BCR-Abl-1 in the docking studies. The experimental process involved the reaction of Ethyl propiolate(cas: 623-47-2Recommanded Product: Ethyl propiolate)
Ethyl propiolate(cas: 623-47-2) is a clear colorless to pale yellow liquid that is soluble in ethanol, ether and chloroform. It an important organic chemical raw material and pharmaceutical intermediate. Ethyl propargylate is obtained by oxidation of propargyl alcohol to propargylic acid followed by esterification.Recommanded Product: Ethyl propiolate
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