Synthesis and evaluation of antitumoral activity of ester and amide derivatives of 2-arylamino-6-trifluoromethyl-3-pyridinecarboxylic acids

Ester and amide derivatives of 2-arylamino-6-trifluoromethyl-3-pyridinecarboxylic acids demonstrated inhibitory effects on the growth of a wide range of cancer cell lines in the low micromolar to nanomolar concentration range. The synthesis and antitumoral activity of ester and amide derivatives of...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2008-03, Vol.16 (5), p.2367-2378
Main Authors: Onnis, Valentina, Cocco, Maria T., Lilliu, Valentina, Congiu, Cenzo
Format: Article
Language:English
Subjects:
Amide derivatives
Amides - chemical synthesis
Amides - chemistry
Amides - pharmacology
Amination
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Antitumoral activity
Biological and medical sciences
Cell Line, Tumor
Cell Survival - drug effects
Ester derivatives
Esters - chemical synthesis
Esters - chemistry
Esters - pharmacology
Fluorine Compounds - chemistry
General aspects
Humans
Medical sciences
Methylation
Molecular Structure
Niacin - chemistry
Pharmacology. Drug treatments
SAR
Sensitivity and Specificity
Structure-Activity Relationship
Synthesis
Trifluoromethylpyridine
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Summary:Ester and amide derivatives of 2-arylamino-6-trifluoromethyl-3-pyridinecarboxylic acids demonstrated inhibitory effects on the growth of a wide range of cancer cell lines in the low micromolar to nanomolar concentration range. The synthesis and antitumoral activity of ester and amide derivatives of 2-arylamino-6-trifluoromethyl-3-pyridinecarboxylic acids 8– 58 is described. Trifluoromethylpyridine derivatives 8– 58 were evaluated for their anticancer activity toward human tumoral cell lines by the National Cancer Institute (NCI). Most of them possess encouraging anticancer activity, having GI 50 values in the low micromolar to nanomolar concentration range. The 3,4,5-trimethoxyphenylamide 44 was the most active, and it is now under review by NCI Biological Evaluation Committee for possible further studies.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2007.11.069