Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363

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Synthesis and Photodynamic Activity of Peri-xanthenoxanthene Derivatives
Yong ChenZheng-quan LiYuan-qiang DengBing-ying YuWen-long Pan Hua-can Song
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論文ID: c19-00240

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Photodynamic therapy (PDT) is a modern cancer therapy. But it is still difficult to obtain ideal photosensitizers. We synthesized six new peri-xanthenoxanthene derivatives rapidly and efficiently using solid-phase carbon-bath microwave irradiation technology, and investigated their in vitro photodynamic antitumor activity with MTT assay. Our results showed that all compounds exhibited extremely low dark cytotoxicity and good phototoxicity against four human cancer cell lines. In particular, compound 3c showed the best in vitro PDT activity against Hela cells and Bel-7402 cells with IC50 values of 91 nmol/L and 74 nmol/L respectively. Its value of 1-octanol/water partition coefficient (logKow) was 0.5309, suggesting that it is a promising photosensitizer for PDT due to its low dark cytotoxicity, high phototoxicity, and potential water solubility.

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© 2019 The Pharmaceutical Society of Japan
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