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Novel design of a pentacyclic scaffold as structural mimic of saframycin A |
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| Authors: | Chi Wi Ong Yu An ChangJing-Yun Wu Chien-Chung Cheng |
| Affiliation: | a Department of Chemistry, National Sun Yat Sen University, Kaoshiung 804, Taiwan, ROC b Chung Chou Institute of Technology, Chang-Hwa 501, Taiwan, ROC c Department of Chemistry, Tamkang University, Tamsui 251, Taiwan, ROC |
| Abstract: | The design, synthesis and evaluation of a pentacyclic scaffold, CWO-324 to mimic saframycin A is described. CWO-324 is readily synthesized in five steps from 1,4-diacetyl-piperazine-2,5-dione and 2,5-dimethoxybenzaldehyde. CWO-324 was found to scission DNA, binds to bases 69-83(5′-GCAGTCAGG CACCGT-3′) of Hind III/Rsa I from plasmid pBR322 DNA in a foot-printing study and possesses anti-tumor activity. |
| Keywords: | 5a,12a-diazapentacene saframycin model DNA binding and scissioning |
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