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

Abdelrahman, Mostafa H.; Ali, Mamdouh M.

doi:10.21608/bfsa.2016.62589

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

Document Type : Original Article

Authors

¹ Department of Organic Chemistry, Faculty of Pharmacy, Al-Azhar University, Assiut 71524, Egypt

² Department of Biochemistry, Division of Genetic Engineering and Biotechnology, National Research Centre, Dokki 12622, Giza, Egypt

10.21608/bfsa.2016.62589

Abstract

A series of novel3-(1H-pyrazol-3-yl)-4H-1,2,4-triazole derivatives were synthesized and the structure of the prepared compounds was fully characterized by ¹H NMR, ¹³C 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 7l and 7o exhibited remarkable anticancer activity similar to or more potent than doxorubicin against breast MCF-7 and Lung A549 cell lines.