公开(公告)号：US20210145968A1

公开(公告)日：2021-05-20

申请号：US16645301

申请日：2018-09-05

申请人： TECHNICAL INSTITUTE OF PHYSICS AND CHEMISTRY OF THE CHINESE ACADEMY OF SCIENCES

发明人： Pengfei WANG ,  Jiasheng WU ,  Weimin LIU ,  Xiuli ZHENG ,  Ying GU

IPC分类号： A61K41/00 ,  C07C225/32 ,  C07C221/00 ,  A61K47/10 ,  C07C229/16 ,  C07C227/28 ,  C07C229/28 ,  C07C243/20 ,  C07C241/02 ,  C07D401/12 ,  C07D403/12 ,  C07D519/00 ,  C07D295/13 ,  C07D295/205 ,  C07C323/30 ,  C07C323/38

摘要： The present invention discloses a hypocrellin derivative substituted both in a peri-position and in a 2-position by an amino, and a preparation method and use thereof. A general structural formula of the derivative is as represented by formulas I-a to I-d: The hypocrellin derivative substituted both in a peri-position and in a 2-position by an amino prepared in the present invention has a maximum absorption wavelength of 600-650 nm and a molar extinction coefficient reaching about 20000-40000 M−1cm−1. Compared with unmodified hypocrellin or hypocrellin having only a 2-position modified, an absorption spectrum of the derivative is significantly red-shifted and the molar extinction coefficient is greatly improved, and the derivative can efficiently produce reactive oxygen species such as singlet oxygen in a photosensitive condition. In the same condition, the hypocrellin derivative substituted both in a peri-position and in a 2-position by an amino involved in the present invention, when used as a photosensitizer, has a stronger ability to photo-dynamically inactivate tumor cells than the first and second generation commercial photosensitizers.