Relationship between cytotoxicity and DNA-binding affinity of amidine derivatives of tetrahydroquino[4,3- b][1]benzazepines and tetrahydrobenzo[ k]naphthyridines

Two sets of amidine derivatives of the non-planar tetracyclic systems: tetrahydroquino[4.3- b][1]benzazepine ( I) and tetrahydrobenzo[ k]naphthyridine ( II), bearing three types of side chains (hydroxyl, amine and alkyl) have been synthesized. All the compounds were found to possess weak but signifi...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1995-12, Vol.5 (24), p.3003-3006
Main Authors: Eifler-Lima, V.L., Uriac, P., Huet, J., Jenkins, T.C., Thurston, D.E.
Format: Article
Language:English
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Summary:Two sets of amidine derivatives of the non-planar tetracyclic systems: tetrahydroquino[4.3- b][1]benzazepine ( I) and tetrahydrobenzo[ k]naphthyridine ( II), bearing three types of side chains (hydroxyl, amine and alkyl) have been synthesized. All the compounds were found to possess weak but significant DNA-binding affinity which correlated with in vitro cytotoxicity across two cell lines. Newly synthesized compounds of series I and II bind to DNA with an affinity corresponding to their cytotoxicity. RCH 2CH 2CH 3, CH 2CH 2CH 2OH CH 2CH 2CH 2NH 2, CH 2CH 2CH 2CH 2NH 2
ISSN:0960-894X
1464-3405
DOI:10.1016/0960-894X(95)00526-9