Akella Venkateswarlu

Novel C-ring analogues of 20(S)-camptothecin. Part 3: synthesis and their in vitro cytotoxicity of A-, B- and C-ring analogues

Several 5-substituted alkoxy 20(S)-camptothecin analogues having A- and B-ring substituents were prepared via semi-synthesis. Most of these compounds were found to exhibit potent anti-cancer activity based on their in vitro cytotoxicity data obtained against human tumor cell lines.

In vitro cytotoxicity of 5-aminosubstituted 20(S)-camptothecins. part 1

A number of 5-aminosubstituted 20(S)-camptothecin analogues were prepared via semi-synthesis starting from 20(S)-camptothecin and 9-methoxy 20(S)-camptothecin. In vitro anti-cancer activity of these analogues was determined using 60 human tumor cell line assay. Although water solubility of most of these compounds was improved compared to 20(S)-camptothecin, their anti-cancer activity was considerably diminished. However, only smaller substituents such as methylamine or hydroxylamine as present in 8s and 8t, respectively, showed good activity with improved water solubility.

Novel C-ring analogues of 20(S)-camptothecin-part-2: synthesis and in vitro cytotoxicity of 5-C-substituted 20(S)-camptothecin analogues.

A series of 5-C-substituted 20(S)-camptothecin analogues were synthesised and evaluated their in vitro anti-cancer activity. Several of these analogues have showed excellent activity against human tumor cell lines.