SYNTHESIS OF NOVEL 2- 1-( 4-METHYLPIPERAZINYL) NICOTINAMIDE DERIVATIVE OF ANTITUMOR ACTIVITY

A NOVEL 2-(1-(4-METHYLPIPERAZINYL)]NICOTINAMIDE DERIVATIVE 5 WAS SYNTHESIZED THROUGH AROMATIC NUCLEOPHILIC SUBSTITUTION REACTION OF 4-METHYLPIPERA/INE WITH 2-BROMONICOTINAMIDE ANALOGUE 4 THE LATTER WAS OBTAINED VIA BROMINATION OF 2-CYANO-A’-PHENYLPENTAMIDE DERIVATIVE 3 IN GLAEIAL ACETIC ACID. MOREOVER, PENTAMIDE 3 WAS PREPARED THROUGH BASE-CATALYZED MICHAEL ADDITION REACTION OF CYANACETANILIDE 2 TO CHALCONC 1 IN REFLUXING ABSOLUTE ETHANOL. ANTITUMOR PROPERTIES OF 5 UTILIZE 59 DIFFERENT HUMAN TUMOR CELL LINES, REPRESENTING LEUKEMIA, MELANOMA AND CANCER OF THE LUNG, COLON, BRAIN, OVARY, BREAST, PROSTATE AS WELL AS KIDNEY WERE SCREENED. REMARKABLE IN VITRO ACTIVITIES (GI50, TGI AND LC5()) AGAINST ALL THE TESTED HUMAN TUMOR CELL LINES WERE OBSERVED.