DERIVATIVES OF HYPOCRELLIN WITH PERI-POSITION AND 2-POSITION SIMULTANEOUSLY SUBSTITUTED BY AMINO GROUPS

摘要

Derivatives of hypocrellin with peri-position and 2-position simultaneously substituted by amino groups and a preparation method and application thereof are disclosed. The structural formula of the derivatives is as shown in the formulae I-a to I-d. The prepared derivatives of hypocrellin with peri-position and 2-position simultaneously substituted by amino groups have a maximum absorption wavelength of 600-650nm, and a molar extinction coefficient of about 20000-40000M ^-1cm ^-1. Compared with unmodified hypocrellin or hypocrellin only modified at 2-position, the prepared derivatives of hypocrellin have a significantly red-shifted absorption spectrum and a greatly enhanced molar extinction coefficient, and can efficiently produce reactive oxygen species such as singlet oxygen under a photosensitive condition. Under the same condition, the derivatives of hypocrellin with peri-position and 2-position simultaneously substituted by amino groups act as photosensitizers, and have higher photodynamic inactivation of tumor cells than the first and second generations of commercial photosensitizers.