Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10591835 | Bioorganic & Medicinal Chemistry Letters | 2014 | 6 Pages |
Abstract
Four series of cassiarin A derivatives with alkanoyl (3a-3d), aroyl (4a-4d), hydroxy/amino-substituted ethylene glycol (5a-5c) and selenium-containing (6a) side chains were synthesized. Their antitumor activities were evaluated against BT474, CHAGO, HepG2, KATO-III, SW620 and CaSki cancer cell lines. Preliminary results demonstrated that 5b had moderate activities against HepG2 and KATO-III cell lines, while 5c showed moderate to high cytotoxicity against most tested cell lines. In addition, 6a exhibited moderate cytotoxicity against cervical cells, CaSki. DNA-binding and ethidium bromide displacement experiments suggested that 5c and 5b binds to DNA via an intercalative mode, whereas 6a did not. However, the selenium-containing cassiarin A derivative 6a inhibited topoisomerase II with more than 95% inhibition at the concentration of 50 μM. These cassiarin A derivatives showed lower toxicity to normal cells, WI-38 than amonafide therefore they are potential lead compounds to be further developed as new anticancer agents.
Keywords
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Urarika Luesakul, Tanapat Palaga, Kuakarun Krusong, Nattaya Ngamrojanavanich, Tirayut Vilaivan, Songchan Puthong, Nongnuj Muangsin,