Design, synthesis and antiproliferative activity evaluation of a series of pyrrolo[2,1-f][1,2,4]triazine derivatives.

ID: ALA4619747

Journal: Bioorg Med Chem Lett

Title: Design, synthesis and antiproliferative activity evaluation of a series of pyrrolo[2,1-f][1,2,4]triazine derivatives.

Authors: Xiang HY, Chen YH, Wang Y, Zhang X, Ding J, Meng LH, Yang CH.

Abstract: A series of 6-aminocarbonyl pyrrolo[2,1-f][1,2,4]triazine derivatives were designed by scaffold hopping strategy. The IC₅₀ values of compound 14a against PI3Ks were measured, showing selective activity against p110α and p110δ with IC₅₀s of 122 nM and 119 nM respectively. All the synthesized compounds were evaluated for their antiproliferative activity against human cancer cells by SRB assay. Compounds 14a, 14p and 14q exhibited potent antiproliferative activity against five types of human cancer cells and the PK property of 14q was also investigated here.

CiteXplore: 32317209

DOI: 10.1016/j.bmcl.2020.127194

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