title: In vitro cytotoxicity of 5-aminosubstituted 20(S)-camptothecins. Part 1.
abstract: 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.
authors.affiliation: Natural Products Division, Dr Reddy's Research Foundation, Miyapur, Hyderabad, AP, India.
authors.forename: D
authors.initials: D
authors.lastname: Subrahmanyam
authors.forename: V M
authors.initials: VM
authors.lastname: Sarma
authors.forename: A
authors.initials: A
authors.lastname: Venkateswarlu
authors.forename: T V
authors.initials: TV
authors.lastname: Sastry
authors.forename: A P
authors.initials: AP
authors.lastname: Kulakarni
authors.forename: D S
authors.initials: DS
authors.lastname: Rao
authors.forename: K V
authors.initials: KV
authors.lastname: Reddy
mesh_terms: 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
chemical_list: D000970:Antineoplastic Agents; D002166:Camptothecin