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Title: Potent antitumor activity of synthetic 1,2-naphthoquinones and 1,4-naphthoquinones
Authors: Ngampong Kongkathip
Boonsong Kongkathip
Pongpun Siripong
Chak Sangma
Suwaporn Luangkamin
Momad Niyomdecha
Suppachai Pattanapa
Suratsawadee Piyaviriyagul
Palangpon Kongsaeree
Kasetsart University
National Cancer Institute Thailand
Mahidol University
Keywords: Biochemistry, Genetics and Molecular Biology;Chemistry;Pharmacology, Toxicology and Pharmaceutics
Issue Date: 17-Jul-2003
Citation: Bioorganic and Medicinal Chemistry. Vol.11, No.14 (2003), 3179-3191
Abstract: Rhinacanthone (1) and two 1,2-pyranonaphthoquinones (2,3) were synthesized and found to show very potent cytotoxicity against three cancer cell lines (KB, HeLa and HepG2) with IC50values of 0.92-9.63 μM, whereas the corresponding hydroxylated derivative 4 had reduced cytotoxicity (IC50values of 7.61-24.13 μM). Three 1,2-furanonaphthoquinone derivatives (5-7) were also synthesized with similar cytotoxicity as 1,2-pyranonaphthoquinones. In comparison to 1,2-naphthoquinones, six 1,4-naphthoquinones derivatives fused with pyran ring (8-10) and furan ring (11-13) were synthesized and they showed less cytotoxicity or inactive to the cancer cell lines. Moreover, compound 13 had significant cytotoxicity against HeLa cell line (IC50value of 9.25 μM) while it showed no toxic to vero cell. © 2003 Elsevier Science Ltd. All rights reserved.
ISSN: 09680896
Appears in Collections:Scopus 2001-2005

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