Camptothecin analogs and methods of preparation thereof

Abstract

The present invention provides generally a compound having the following general formula (1): wherein Rand Rare independently the same or different and are hydrogen, an alkyl group, an alkenyl group, a benzyl group, an alkynyl group, an alkoxyl group, an aryloxy group, an acyloxy group, a carbonyloxy group, a carbamoyloxy group, a halogen, a hydroxyl group, a nitro group, a cyano group, an azido group, a formyl group, a hydrazino group, an acyl group, an amino group, —SR, wherein, Ris hydrogen, an acyl group, an alkyl group, or an aryl group, or Rand Rtogether form a group of the formula —O(CH)O— wherein n represents the integer 1 or 2; Ris H, F, a halogen atom, a nitro group, an amino group, a hydroxyl group, or a cyano group; or Rand Rtogether form a group of the formula —O(CH)O— wherein n represents the integer 1 or 2; Ris H, F, a Calkyl group, a Calkenyl group, a Calkynyl group, or a Calkoxyl group; Ris a Calkyl group, or a propargyl group; and R, Rand Rare independently a Calkyl group, a Calkenyl group, a Calkynyl group, an aryl group or a —(CH)Rgroup, wherein N is an integer within the range of 1 through 10 and Ris a hydroxyl group, alkoxy group, an amino group, an alkylamino group, a dialkylamino group, a halogen atom, a cyano group or a nitro group; and pharmaceutically acceptable salts thereof.