SYNTHESIS AND IN VITRO ANTITUMOR ACTIVITY OF SOME FUSED PYRAZOLE AND PYRAZOLINE RING SYSTEMS

This research work describes the synthesis of some pyrazole and pyrazoline fused ring systems substituted with variable biologically-active chemical species. All of the newly synthesized target compounds were selected by the NCI for in-vitro antitumor screening. Six compounds namely, 3, 4a,b, 5a,b and 9a have passed successfully through the primary 3-cell line assay and were promoted for the full panel 60-cell line assay. These active compounds exhibited broad spectrum of antitumor activity against most of the tested tumor cell lines. Compound 5a proved to be the most active antitumor agent in the present study with GI50, TGI and LC50 MG-MID values of 8.12, 25.7 and 69.2 µM, respectively, with high sensitivity towards some leukemia, melanoma and renal cell lines. The other five active compounds showed variable degrees of appreciable antitumor activity (GI50 and TGI MG-MID values range 14.1- 19.5 and 38.0-53.7 µM, respectively)