| Literature DB >> 23353747 |
Suthananda N Sunassee1, Clinton G L Veale, Nelusha Shunmoogam-Gounden, Omalaja Osoniyi, Denver T Hendricks, Mino R Caira, Jo-Anne de la Mare, Adrienne L Edkins, Antônio V Pinto, Eufrânio N da Silva Júnior, Michael T Davies-Coleman.
Abstract
Naphthoquinones have been found to have a wide range of biological activities, including cytotoxicity to cancer cells. The secondary metabolites lapachol, α- and β-lapachone and a series of 25 related synthetic 1,4-naphthoquinones were screened against the oesophageal cancer cell line (WHCO1). Most of the compounds exhibited enhanced cytotoxicity (IC50 1.6-11.7 μM) compared to the current drug of choice cisplatin (IC50 = 16.5 μM). This study also established that the two new synthetic halogenated compounds 12a and 16a (IC50 = 3.0 and 7.3 μM) and the previously reported compound 11a (IC50 = 3.9 μM), were non-toxic to NIH3T3 normal fibroblast cells. Cell death of oesophageal cancer cells by processes involving PARP cleavage caused by 11a was shown to be associated with elevated c-Jun levels, suggesting a role for this pathway in the mechanism of action of this cohort of naphthoquinone compounds.Entities:
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Year: 2013 PMID： 23353747 DOI： 10.1016/j.ejmech.2012.12.048
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 7.088