Synthesis and evaluation of anticancer activity of 2-arylamino-6-trifluoromethyl-3-(hydrazonocarbonyl)pyridines.

Abstract

The synthesis and anticancer activity of 2-arylamino-6-trifluoromethyl-3-(hydrazonocarbonyl)pyridines is described. The new trifluoromethylpyridine derivatives were evaluated for their anticancer activity toward human cancer cell lines by the National Cancer Institute (NCI). Most of them had excellent growth inhibition activity, having GI(50) values in the low micromolar to nanomolar concentration range. The most potent 2,6-dichlorobenzaldehydehydrazone 29 inhibited the growth of all tested cancer cell lines with nanomolar potency, and did not show animal toxicity. Hydrazone 29 has been selected by the Biological Evaluation Committee of NCI for testing in vivo Hollow Fiber Assay.

• Authors: Valentina Onnis, Maria T Cocco, Roberta Fadda, Cenzo Congiu
• Journal: Bioorganic & medicinal chemistry (Bioorg Med Chem) Vol. 17 Issue 17 Pg. 6158-65 (Sep 01 2009) ISSN: 1464-3391 [Electronic] England
• PMID: 19679483 (Publication Type: Journal Article)

Chemical References

• Antineoplastic Agents
• Hydrazines
• Pyridines
• trifluoromethylpyridine

Topics

• Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
• Cell Line, Tumor
• Drug Screening Assays, Antitumor
• Humans
• Hydrazines (chemical synthesis, chemistry, pharmacology)
• Pyridines (chemical synthesis, chemistry, pharmacology)
• Structure-Activity Relationship