Abstract:
:20(S)-Camptothecin derivatives having nitro, amino, chloro, bromo, hydroxyl and methoxyl groups in the A-ring were synthesized. B-Ring hydrogenated camptothecin (2a) was converted into 10-hydroxycamptothecin (6e) by treatment with lead tetraacetate in trifluoroacetic acid. 10-Substituted derivatives (6) were obtained by a photoreaction of N-oxides (9). The cytotoxicity of the A-ring modified camptothecins was evaluated against KB cells in vitro and leukemia L1210 in mice. 7-Ethyl-10-hydroxycamptothecin (6i) was identified as a potential derivative for further modification.
journal_name
Chem Pharm Bull (Tokyo)journal_title
Chemical & pharmaceutical bulletinauthors
Sawada S,Matsuoka S,Nokata K,Nagata H,Furuta T,Yokokura T,Miyasaka Tdoi
10.1248/cpb.39.3183subject
Has Abstractpub_date
1991-12-01 00:00:00pages
3183-8issue
12eissn
0009-2363issn
1347-5223journal_volume
39pub_type
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