Synthesis and evaluation of antitumoral activity of ester and amide derivatives of 2-arylamino-6-trifluoromethyl-3-pyridinecarboxylic acids.
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.
Onnis
Valentina
V
Dipartimento di Tossicologia, Università degli Studi di Cagliari, via Ospedale 72, Cagliari I-09124, Italy.
Cocco
Maria T
MT
Lilliu
Valentina
V
Congiu
Cenzo
C
D000577:Amides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000586:Amination; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004952:Esters / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D017611:Fluorine Compounds / Q000737:chemistry; D006801:Humans; D008745:Methylation; D015394:Molecular Structure; D009525:Niacin / Q000737:chemistry*; D012680:Sensitivity and Specificity; D013329:Structure-Activity Relationship
D000577:Amides; D000970:Antineoplastic Agents; D004952:Esters; D017611:Fluorine Compounds; D009525:Niacin