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Design and Synthesis of Pyridazine Containing Compounds with Promising Anticancer Activity.
- Source :
-
Chemical & pharmaceutical bulletin [Chem Pharm Bull (Tokyo)] 2017; Vol. 65 (3), pp. 236-247. - Publication Year :
- 2017
-
Abstract
- Certain pyridazine containing compounds 2a-f, 3a, b, 4a, b, 5a, b, 6a and b were synthesized and characterized by spectroscopic means and elemental analysis. All the synthesized compounds were screened for their cytotoxic activity in vitro on colon cancer cell line (HCT-116) and breast cancer cell line (MCF-7). In addition, the antitumor activity of the synthesized compounds was tested in vivo against Ehrlich's ascites carcinoma (EAC) solid tumor grown in mice. The in vitro vascular endothelial growth factor receptor (VEGFR) enzyme inhibition assay was carried out for the most active compounds at a single dose of 10 µM. The obtained results revealed that compound 5b, which showed potent cytotoxic activity against HCT-116 also, exhibited the highest inhibition in the VEGFR kinase assay (92.2%).
- Subjects :
- Animals
Antineoplastic Agents chemistry
Cell Proliferation drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Female
HCT116 Cells
Humans
MCF-7 Cells
Mice
Models, Molecular
Molecular Structure
Neoplasms, Experimental drug therapy
Neoplasms, Experimental pathology
Protein Kinase Inhibitors chemical synthesis
Protein Kinase Inhibitors chemistry
Pyridazines chemical synthesis
Pyridazines chemistry
Receptors, Vascular Endothelial Growth Factor antagonists & inhibitors
Receptors, Vascular Endothelial Growth Factor metabolism
Structure-Activity Relationship
Antineoplastic Agents chemical synthesis
Antineoplastic Agents pharmacology
Drug Design
Protein Kinase Inhibitors pharmacology
Pyridazines pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1347-5223
- Volume :
- 65
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- Chemical & pharmaceutical bulletin
- Publication Type :
- Academic Journal
- Accession number :
- 28250345
- Full Text :
- https://doi.org/10.1248/cpb.c16-00532