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Relationship between cytotoxicity and DNA-binding affinity of amidine derivatives of tetrahydroquino[4,3-b][1]benzazepines and tetrahydrobenzo[k]naphthyridines |
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| Authors: | V L Eifler-Lima P Uriac J Huet T C Jenkins D E Thurston |
| Institution: | a Laboratoire de Chimie Pharmaceutique, Faculté de Pharmacie, Avenue Pr L.Bernard 35043, Rennes -, France b Present address: Curso de Pos-Graduaçao em Ciências Farmacêuticas, Faculdade de Farmacia-UFRGS, Av. Ipiranga 2752, Porto Alegre RS -, Brazil c CRC Biomolecular Structure Unit, The Institute of Cancer Research, Sutton, Surrey, SM2 5NG, UK d School of Pharmacy and Biomedical Science, University of Portsmouth, Park Building, King Henry 1st Street, Portsmouth, Hants. PO1 2DZ, United Kingdom |
| Abstract: | Two sets of amidine derivatives of the non-planar tetracyclic systems: tetrahydroquino4.3-b]1]benzazepine (I) and tetrahydrobenzok]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. |
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