Morgan A R, Rampersaud A, Garbo G M, Keck R W, Selman S H
Department of Chemistry, College of Arts and Science, University of Toledo, Ohio 43606.
J Med Chem. 1989 Apr;32(4):904-8. doi: 10.1021/jm00124a029.
Purpurins are a class of porphyrin derivative that have been shown to have good in vivo cytotoxicity to N-[4-(5-nitro-2-furyl)-2-thiazolyl]formamide (FANFT) induced rat bladder tumors (AY-27) implanted into Fisher 344 rats. The synthesis of purpurins from etioporphyrin I and coproporphyrin I proceeds in high yield and with a high degree of regioselectivity. Product formation can be rationalized in terms of relief of steric strain about the periphery of the purpurin macrocycle. The effect of therapeutic light doses using the rat footpad model suggests that, at therapeutic sensitizer doses, normal tissue damage is within acceptable limits, particularly for metalated purpurins.
紫红素是一类卟啉衍生物，已证明其对植入Fisher 344大鼠体内的N-[4-(5-硝基-2-呋喃基)-2-噻唑基]甲酰胺（FANFT）诱导的大鼠膀胱肿瘤（AY-27）具有良好的体内细胞毒性。由初卟啉I和粪卟啉I合成紫红素的产率很高，且具有高度的区域选择性。产物的形成可以从紫红素大环外围空间张力的缓解来解释。使用大鼠足垫模型的治疗光剂量效果表明，在治疗敏化剂剂量下，正常组织损伤在可接受范围内，特别是对于金属化紫红素而言。
