ChemInform Abstract: CONFORMATIONS, DNA BINDING PARAMETERS, AND ANTILEUKEMIC ACTIVITY OF CERTAIN CYTOTOXIC PROTOBERBERINE ALKALOIDS

Autor:	Frederick W. Dekow, Mark Cushman, Linda B. Jacobsen
Rok vydání:	1979
Předmět:	chemistry.chemical_compound chemistry In vivo Stereochemistry Diastereomer Cytotoxic T cell Alcohol Equilibrium dialysis General Medicine P388 leukemia In vitro DNA
Zdroj:	Chemischer Informationsdienst. 10
ISSN:	0009-2975
DOI:	10.1002/chin.197928329
Popis:	The tetrahydroprotoberberine alkaloids 5 and 7 possessing a trans-quinolizidine conformation display in vitro KB cytotoxicities in contrast to their corresponding diastereomers 4 and 6 which exist in the cis-quinolizidine conformation and are much less toxic. The DNA-binding parameters of these compounds as well as the protoberberine salts 1, 8, and 9 have been examined by equilibrium dialysis. Only the quaternary salts bind to DNA. The alcohol 5 showed low in vivo activity against leukemia P388 systems, while the quaternary salts 8 and 9 proved to be toxic to the host.
Databáze:	OpenAIRE
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