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.
Subrahmanyam
D
D
Natural Products Division, Dr Reddy's Research Foundation, Miyapur, Hyderabad, AP, India.
Sarma
V M
VM
Venkateswarlu
A
A
Sastry
T V
TV
Kulakarni
A P
AP
Rao
D S
DS
Reddy
K V
KV
D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D002166:Camptothecin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D015394:Molecular Structure; D012995:Solubility; D013057:Spectrum Analysis; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D002166:Camptothecin