☆ 4.7 Article

Triazolopyridazine derivatives: Synthesis, cytotoxic evaluation, c-Met kinase activity and molecular docking

BIOORGANIC CHEMISTRY (2019)

Journal

BIOORGANIC CHEMISTRY

Volume 92, Issue -, Pages -

Publisher

ACADEMIC PRESS INC ELSEVIER SCIENCE

DOI: 10.1016/j.bioorg.2019.103272

Keywords

Triazolopyridazines; Pyridazines; Cytotoxic activity; c-Met kinase

Categories

Biochemistry & Molecular Biology Chemistry, Organic

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Abstract

Novel series of some triazolo [4,3-b]pyridazine derivatives were designed and synthesized. All the newly synthesized compounds were evaluated for their cytotoxic activity at 10(-5) M concentration towards 60 cancer cell lines according to USA NCI protocol. Most of the synthesized compounds showed good activity against SR (leukemia) cell panel. The most active compounds, 2f and 4a were subjected for further evaluation at a five dose level screening and their efficacy for c-Met kinase inhibition was determined in vitro. Binding mode of these derivatives was explored via molecular docking.

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