3-[(6-Arylamino)pyridazinylamino]benzoic acids: design, synthesis and in vitro evaluation of anticancer activity

A series of novel substituted 3,6-disubstituted pyridazines based on the structure of vatalanib (PTK787) were designed and synthesized. The cytotoxicity of the final compounds was tested in vitro on HT-29 colon cancer cell line. Compounds 2a and 2b with 4-chlorophenylamino moiety, exerted the highes...

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Bibliographic Details
Published in:Archives of pharmacal research 2013, 36(1), , pp.41-50
Main Authors: Abouzid, Khaled A. M., Khalil, Nadia A., Ahmed, Eman M., Mohamed, Khaled Omar
Format: Article
Language:English
Subjects:
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Cell Survival - drug effects
Drug Design
Drug Screening Assays, Antitumor
HT29 Cells
Humans
Medicine
Molecular Docking Simulation
Molecular Structure
Pharmacology/Toxicology
Pharmacy
Phthalazines - chemistry
Phthalazines - pharmacology
Pyridazines - chemical synthesis
Pyridazines - chemistry
Pyridazines - pharmacology
Pyridines - chemistry
Pyridines - pharmacology
Research Article
Structure-Activity Relationship
약학
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Summary:A series of novel substituted 3,6-disubstituted pyridazines based on the structure of vatalanib (PTK787) were designed and synthesized. The cytotoxicity of the final compounds was tested in vitro on HT-29 colon cancer cell line. Compounds 2a and 2b with 4-chlorophenylamino moiety, exerted the highest cytotoxic activity with IC 50 values equal to 15.3 and 3.9 μM respectively. The most promising compound, 2b , was found to be about fivefold more active than vatalanib against HT-29 colon cancer cell line.
ISSN:0253-6269
1976-3786
DOI:10.1007/s12272-013-0007-8