Please use this identifier to cite or link to this item: http://hdl.handle.net/10397/24538
Title: Oxoisoaporphine alkaloid derivatives : synthesis, DNA binding affinity and cytotoxicity
Authors: Tang, H
Wang, XD
Wei, YB
Huang, SL
Huang, ZS
Tan, JH
An, LK
Wu, JY 
Chan, ASC
Gu, LQ
Keywords: Cytotoxicity
DNA binding
Oxoisoaporphine alkaloid derivatives
Synthesis
Issue Date: 2008
Publisher: Elsevier Masson
Source: European journal of medicinal chemistry, 2008, v. 43, no. 5, p. 973-980 How to cite?
Journal: European journal of medicinal chemistry 
Abstract: A series of novel oxoisoaporphine alkaloid derivatives, 9-aminoalkanamido-1-azabenzanthrone (general formula Ar-NHCO(CH 2) nNR 2, Ar = 1-azabenzanthrone, n = 1, 2 or 3), had been synthesized. Compared with 1-azabenzanthrone, the derivatives had significantly higher DNA binding affinity with calf thymus DNA, and higher potent cytotoxicity against different tumor cell lines. The cytotoxicity and the structure-activity relationship of the prepared compounds were studied. The derivatives with two methylene groups (n = 2), and piperidine or ethanolamine functional group in the side chain exhibited highest DNA binding affinity and cytotoxicity.
URI: http://hdl.handle.net/10397/24538
ISSN: 0223-5234
EISSN: 1768-3254
DOI: 10.1016/j.ejmech.2007.07.004
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