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Design and Synthesis of Pyridazine Containing Compounds with Promising Anticancer Activity.

Authors :
Elmeligie S
Ahmed EM
Abuel-Maaty SM
Zaitone SA
Mikhail DS
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%).

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