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Triazolopyridazine derivatives: Synthesis, cytotoxic evaluation, c-Met kinase activity and molecular docking.
- Source :
-
Bioorganic chemistry [Bioorg Chem] 2019 Nov; Vol. 92, pp. 103272. Date of Electronic Publication: 2019 Sep 10. - Publication Year :
- 2019
-
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 <superscript>-5</superscript> 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.<br /> (Copyright © 2019 Elsevier Inc. All rights reserved.)
- Subjects :
- Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Cell Proliferation drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Humans
Molecular Structure
Protein Kinase Inhibitors chemical synthesis
Protein Kinase Inhibitors chemistry
Proto-Oncogene Proteins c-met metabolism
Pyridazines chemical synthesis
Pyridazines chemistry
Structure-Activity Relationship
Tumor Cells, Cultured
Antineoplastic Agents pharmacology
Molecular Docking Simulation
Protein Kinase Inhibitors pharmacology
Proto-Oncogene Proteins c-met antagonists & inhibitors
Pyridazines pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1090-2120
- Volume :
- 92
- Database :
- MEDLINE
- Journal :
- Bioorganic chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 31539742
- Full Text :
- https://doi.org/10.1016/j.bioorg.2019.103272