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
Source :: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2020 Jun 15; Vol. 30 (12), pp. 127194. Date of Electronic Publication: 2020 Apr 13.
Publication Year :: 2020
Abstract: A series of 6-aminocarbonyl pyrrolo[2,1-f][1,2,4]triazine derivatives were designed by scaffold hopping strategy. The IC <subscript>50</subscript> values of compound 14a against PI3Ks were measured, showing selective activity against p110α and p110δ with IC <subscript>50</subscript> s 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.<br />Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.<br /> (Copyright © 2020 Elsevier Ltd. All rights reserved.)

Subjects :: Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Cell Line, Tumor
Cell Proliferation drug effects
Class I Phosphatidylinositol 3-Kinases antagonists & inhibitors
Class I Phosphatidylinositol 3-Kinases metabolism
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Humans
Molecular Structure
Protein Kinase Inhibitors chemical synthesis
Protein Kinase Inhibitors chemistry
Structure-Activity Relationship
Triazines chemical synthesis
Triazines chemistry
Antineoplastic Agents pharmacology
Drug Design
Protein Kinase Inhibitors pharmacology
Triazines pharmacology

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