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标题：Synthesis and Photodynamic Activity of Peri-xanthenoxanthene Derivatives
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作者：Yong Chen ; Zheng-quan Li ; Yuan-qiang Deng 等
期刊名称：Chemical and Pharmaceutical Bulletin
印刷版ISSN：0009-2363
电子版ISSN：1347-5223
出版年度：2019
卷号：67
期号：7
页码：690-692
DOI：10.1248/cpb.c19-00240
出版社：The Pharmaceutical Society of Japan
摘要：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 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (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 and 74 nmol/L, respectively. Its value of 1-octanol/water partition coefficient (log K ow) was 0.5309, suggesting that it is a promising photosensitizer for PDT due to its low dark cytotoxicity, high phototoxicity, and potential water solubility.
关键词：photodynamic therapy (PDT);peri-xanthenoxanthene;antitumor;3-(4;5-dimethylthiazol-2-yl)-2;5-diphenyltetrazolium bromide (MTT) assay;1-octanol;water partition