SYNTHESIS OF CERTAIN ACRIDINE DERIVATIVES OF ANTICIPATED ANTITUMOR AND ANTI-HIV-1 ACTIVITIES

Abstract

In the present investigation, 3 known starting compounds and 43 final compounds belonging to four series of new acridine derivatives of anticipated antitumor and anti-HIV-1 activities have been synthesized. The first and second series belong to the 9-anilinoacridine-2-carboxamide de­ rivatives . The third comprises of 9-oxo-9,10-dihydroacridine-2-carboxamide deriva­ tives, while the last one includes the 9-aminoacridine-2-carboxamide derivatives of similar substitution pattern . The rationale behind the synthesis of these compounds, their methods of synthesis as well as their antitumor and anti-HIV-1 activity are discussed. In this thesis, the following compounds were prepared : 1- known starting and intermediate compounds 1) 4-(2-Carboxyphenyl)aminobenzoic acid . 2) 9-0xo-9,10-dihydroacridine-2-carboxylic acid. 3) 9-Chloroacridine-2-carbonyl chloride. 2- Final compounds 1) 9-(4-Sulfamoylphenyl)aminoacridine-2-yi-N-(4-sulfamoylphenyl)carboxamide 2) 9-(4-Amidinosulfamoylphenyl)aminoacridine-2-yi-N-(4-amidinosulfamoyl phenyl) carboxamide .