Synthesis of 3,3,3-trifluoroethyl isocyanate, carbamate and ureas. Anticancer activity evaluation of -(3,3,3-trifluoroethyl)-'-substituted ureas.

A new method is described for producing 3,3,3-trifluoroethyl isocyanate from perfluoroisobutene (PFIB). Isocyanate was used for synthesis of carbamates and ureas. A series of trifluoroethyl-substituted ureas has been tested in the National Cancer Institute (NCI, Bethesda, USA) by the NCI-60 DTP Human Tumor Cell Line Screening Program at a single high dose (10 M).

Synthesis and anticancer activity evaluation of 3,4-mono- and bicyclosubstituted -(het)aryl trifluoromethyl succinimides.

Novel trifluoromethylated mono- and bicyclic succinimides derived from trifluoromethylmaleic anhydride were synthesized using cyclopentadiene or 2,3-dimethylbutadiene and (het)arylamines. The biological activity of these compounds was evaluated using prediction methods and experimental studies. This series of new trifluoromethyl succinimides ( and ) were tested by the National Cancer Institute (NCI, Bethesda, USA) by Program NCI-60 DTP Human Tumor Cell Line Screen at a single high dose (10 M).

Synthesis, evaluation of anticancer activity and COMPARE analysis of N-bis(trifluoromethyl)alkyl-N'-substituted ureas with pharmacophoric moieties.

A series of new synthesized N-bis(trifluoromethyl)alkyl-N'-substituted ureas have been tested in the National Cancer Institute (NCI, Bethesda, USA) by Program NCI-60 DTP Human Tumor Cell Line Screen at a single high dose (10(-5) M). COMPARE analysis has been carried out for all tested compounds. The tested compounds showed antitumor activity against individual cell lines.

Anticancer activity of N-bis(trifluoromethyl)alkyl-N'-(polychlorophenyl) and N'-(1,2,4-triazolyl) ureas.

A number of N-bis(trifluoromethyl)alkyl-N'-substituted ureas have been synthesized and evaluated for their in vitro anticancer activity against the human cancer cell lines at the National Cancer Institute (NCI, USA). Marked activity was shown for compounds 4a and 5a. The most sensitive cell lines relative to the tested compounds were: 4a UO-31 (renal cancer, logGI(50) -5.

Synthesis and anticancer activity of N-bis(trifluoromethyl)alkyl-N'-thiazolyl and N-bis(trifluoromethyl)alkyl-N'-benzothiazolyl ureas.

A number of N-bis(trifluoromethyl)alkyl-N'-thiazolyl and -benzothiazolyl ureas have been synthesized and evaluated for their in vitro antiproliferative activities against the human cancer cell lines at the National Cancer Institute (NCI, USA). The activity was shown for compounds 8a,c and 9a-c. The most sensitive cell lines relative to the tested compounds are: 8c PC-3 (prostate cancer, logGI(50) -7.

Effect of alkyl substituents on excited state intramolecular proton transfer dynamics of jet-cooled bis(benzoxazolyl)phenoles.

Structural factors affecting the dynamics of the excited state intramolecular proton transfer (ESIPT) are studied for alkyl derivatives of 2,5-bis(2-benzoxazolyl)phenol. Two fluorescence bands with equal decay times are observed in solution, while only one--emitted by the phototautomer--in supersonic jet. All evidence indicates the existence of a potential barrier in the S(1) state.