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

Autor: Subrahmanyam D; Natural Products Division, Dr Reddy's Research Foundation, Miyapur, Hyderabad, AP, India., Sarma VM, Venkateswarlu A, Sastry TV, Kulakarni AP, Rao DS, Reddy KV
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry [Bioorg Med Chem] 1999 Sep; Vol. 7 (9), pp. 2013-20.
DOI: 10.1016/s0968-0896(99)00130-3
Abstrakt: 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.
Databáze: MEDLINE