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.
本发明公开了一种在周位和 2 位均被
氨基取代的
次黄嘌呤衍
生物及其制备方法和用途。该衍
生物的一般结构式如式 I-a 至 I-d 所示:
本发明制备的在周位和 2 位被
氨基取代的
次黄嘌呤衍
生物的最大吸收波长为 600-650 nm,摩尔消光系数约为 20000-40000 M-1cm-1。与未修饰的
次黄嘌呤或仅修饰了 2 位的
次黄嘌呤相比,该衍
生物的吸收光谱明显红移,摩尔消光系数大大提高,在光敏条件下能有效地产生活性氧,如单线态氧。在相同的条件下,本发明中被
氨基取代了周位和 2 位的
次黄嘌呤衍
生物在用作光敏剂时,与第一代和第二代商业光敏剂相比,具有更强的光动力灭活肿瘤细胞的能力。