SYNTHESIS OF NOVEL PYRAZOLE DERIVATIVES BEARING 1,2,4-TRIAZOLE MOIETY AS POTENTIAL ANTICANCER AGENTS

摘要

A series of novel 3-(1H-pyrazol-3-yl)-4H-1,2,4-thazole derivatives were synthesized and the structure of the prepared compounds was fully characterized by ~1H NMR, ~(13)C NMR, and HRESI-MS. Six of the prepared compounds were screened for in-vitro cytotoxicity against different cancer cell lines at National Cancer Institute (NCI), USA. Compound 7e exhibited a broad-spectrum of anticancer activity against different cancer cell lines without pronounced selectivity. Moreover, the anticancer activity of the prepared compounds was also evaluated against different human cancer cell lines including breast MCF-7, lung A549 as well as the human normal melanocyte (HFB4) using doxorubicin as a reference drug. Compounds 71 and 7o exhibited remarkable anticancer activity similar to or more potent than doxorubicin against breast MCF-7 and Lung AS49 cell lines.E-mail: mhamedl02004@yahoo.com