| Autor: |
T, Shioiri, T, Aoyama, N, Yamagami, N, Shimizu, N, Mori, K, Kohda |
| Rok vydání: |
1995 |
| Předmět: |
|
| Zdroj: |
Anti-cancer drug design. 10(2) |
| ISSN: |
0266-9536 |
| Popis: |
Tilivalline (TV) possesses a pyrrolo[1,4]benzodiazepine nucleus and an indole substituent in its structure, and is cytotoxic toward mouse leukemia L1210 cells. In order to obtain more effective compounds, we have previously synthesized a variety of TV analogues. In this study, the cytotoxicity of these compounds has been evaluated. Among the compounds tested, the 11-beta-cyano compound, a TV analogue bearing the cyano group instead of the indole group, is approximately 100 times more cytotoxic than TV itself. The alpha-epimer of this cyano compound has about one-hundredth the cytotoxicity of the 11-beta-cyano compound. Structure-cytotoxicity relationships are discussed, including the effects of stereoisomers (alpha and beta) at the 11 position and substitution at the benzene moiety of TV. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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