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. The most sensitive cell lines relative to the tested compounds are: 5g Leukemia RPMI-8226 (GI% 52.7), Non-Small Cell Lung cancer HOP-92 (GI % 88.53), NCI-H522 (GI % 64.41), Melanoma UACC-62 (GI% 53.08), SK-MEL-5 (GI % 74.63), Breast cancer MDA-MB-468 (GI% 51.29), T-47D (GI % 65.1), 5b Leukemia K-562 (GI % 55.55), 7m Leukemia HL-60(TB) (GI % 51.76).

Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slideHighlights► Novel 17 N-bis(trifluoromethyl)alkyl-N’-substituted ureas were synthesized. ► Synthesized compounds were evaluated by the NCI at a single high dose (10−5 M). ► For all tested compounds COMPARE analysis was carried out. ► The ureas with pharmacophoric moieties demonstrated activity against individual cancer cell lines.