Chemical and Pharmaceutical Bulletin p. 3183 - 3188 (1991)
Update date:2022-08-04
Topics: Synthesis Derivatives Antitumor Activity
Sawada
Matsuoka
Nokata
Nagata
Furuta
Yokokura
Miyasaka
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.
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