Produção Nacional
Revisado por pares
(Phenylamino)pyrimidine-1,2,3-triazole derivatives as analogs of imatinib: searching for novel compounds against chronic myeloid leukemia
2021; Beilstein Institute for the Advancement of Chemical Sciences; Volume: 17; Linguagem: Inglês
10.3762/bjoc.17.144
ISSN2195-951X
AutoresLuiz Cláudio Ferreira Pimentel, Lucas Villas Bôas Hoelz, Henayle Fernandes Canzian, Frederico Silva Castelo Branco, Andressa Paula de Oliveira, Vinícius R. Campos, Floriano Paes Silva Júnior, Rafael Ferreira Dantas, Jackson A. L. C. Resende, Anna C. Cunha, Núbia Boechat, Mônica M. Bastos,
Tópico(s)Eosinophilic Disorders and Syndromes
ResumoThe enzyme tyrosine kinase BCR-Abl-1 is the main molecular 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 biologically 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 IC
Referência(s)