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.

Synthesis and in vitro antitumoral activity of new 3,5-dicyanopyridine derivatives.

A new series of 2-amino-4-aryl-6-dialkylamino-3,5-dicyanopyridines, 20-47, were synthesized in satisfactory overall yield, through a simple synthetic strategy using 3-amino-3-(dialkylamino)-propenenitriles 1 and 2 as key intermediates. 3,5-Dicyanopyridine derivatives 20-47 were evaluated for their in vitro anticancer activity toward cell lines of nine different types of human cancers. Some of the newly prepared compounds demonstrated inhibitory effects on the growth of a wide range of cancer cell lines generally at 10(-6) M level and in some cases at 10(-8) M concentration.

Amidrazones as precursors of biologically active compounds--synthesis of diaminopyrazoles for evaluation of anticancer activity.

The regioselectivity of coupling phenyl isocyanate to 3-(2-acylhydrazino)-3-aminopropenenitriles and ethyl 3-(2-acylhydrazino)-3-aminopropenoates as simple access to aminopyrazole derivatives, endowed with potential antitumoral activity, is reported. 3-(2-Acylhydrazino)-3-aminopropenenitriles react with phenyl isocyanate to afford 3-amino-3-(2-acylhydrazino)-2-phenylaminocarbonyl-2-propenenitriles. These key intermediates were cyclized into 3,5-diaminopyrazole-4-carboxamide derivatives.

New potential anticancer agents based on the anthranilic acid scaffold: synthesis and evaluation of biological activity.

The synthesis and anticancer activity of new compounds designed on the anthranilic acid scaffold are reported. The antiproliferative activity was assayed by the National Cancer Institute in established in vitro and in vivo anticancer experimental models. Structural variations based on the flufenamic acid motif afforded a series of (hetero)aryl esters of N-(2-(trifluoromethyl)pyridin-4-yl)anthranilic acid, which showed in vitro growth inhibitory properties against human tumor cell lines in nanomolar to low micromolar concentrations.

Synthesis and in vitro antitumoral activity of new hydrazinopyrimidine-5-carbonitrile derivatives.

A new series of 2-amino-6-(2-alkyl or arylidenehydrazinyl)-4-(dialkylamino)pyrimidine-5-carbonitriles, 5-24, were synthesized in satisfactory overall yield, using 2-amino-4-(dialkylamino)-6-hydrazino-5-pyrimidinecarbonitriles 3, 4, as key intermediates, by applying classical synthetic methods to construct the hydrazone moiety at C-6 of the pyrimidine ring. Hydrazinopyrimidine derivatives 5-24 were evaluated for their in vitro anticancer activity toward cell lines of nine different types of human cancers. Some of the newly prepared compounds demonstrated inhibitory effects on the growth of a wide range of cancer cell lines generally at 10(-5)M level and in some cases at 10(-7)M concentrations.

Synthesis and antiproliferative activity of 2,6-dibenzylamino-3,5-dicyanopyridines on human cancer cell lines.

A new series of 2,6-dibenzylamino-3,5-dicyanopyridines were synthesized and evaluated for their in vitro anticancer activity toward cell lines of nine different types of human cancer. Some of newly prepared compounds demonstrated remarkable anticancer activity against most of the tested subpanel tumor cell lines.

Synthesis of new N-(2-(trifluoromethyl)pyridin-4-yl)anthranilic acid derivatives and their evaluation as anticancer agents.

The N-(2-(trifluoromethyl)pyridin-4-yl)anthranilic acid 6 and a series of its ester and amide derivatives were synthesized and evaluated for their in vitro cytotoxic activity against human cancer cells. Ester derivatives 13 and 18 exhibited potent growth inhibitory activity with GI(50) values at nanomolar concentrations. Among amide derivatives, N-anthraniloylglycinate 19 shown moderate inhibitory activity in the full panel cancer cell line screening.