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个人信息Personal Information
教授
博士生导师
硕士生导师
性别：男
毕业院校：日本富山医科药科大学
学位：博士
所在单位：化工学院
学科：药物化学. 药物分析学
办公地点：西部新校区G-302室（制药科学与技术学院）
联系方式：84986195
电子邮箱：zyzhao@dlut.edu.cn
Synthesis and in vitro phototoxicity of novel pi-extension derivatives of chlorin e6
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论文类型：期刊论文
发表时间：2017-12-07
发表刊物：NEW JOURNAL OF CHEMISTRY
收录刊物：SCIE
卷号：41
期号：23
页面范围：14279-14287
ISSN号：1144-0546
摘要：Six novel E-32-aryl substituted chlorins (5a-5f) were synthesized via improved regioselective bromination and Suzuki-Miyaura cross-coupling reactions with chlorin e6 (1) as a starting material. All the p-extension photosensitizers 5a-5f exhibited significant bathochromic-shifts (ca. 10 nm) in the far red part of the spectrum called the phototherapeutic window and decreased photobleaching under irradiation of 660 nm light. Moreover, 5a-5f possessed higher phototoxicity in vitro against HepG2 cells (IC50 = 0.73 +/- 0.04, 2.33 +/- 0.22, 0.78 +/- 0.05, 0.50 +/- 0.04, 2.25 +/- 0.16 and 0.65 +/- 0.11 mu M, respectively) compared with chlorin e6 (IC50 = 28.9 +/- 1.2 mu M). The enhanced cellular uptake and reactive oxygen species (ROS) production of modified chlorins were found to be responsible for their increased in vitro phototoxicity.
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