Bär V, Erdélyi V, Foris G, Pollák Z, Eckhardt S
Neoplasma. 1977;24(3):253-8.
The evidence of free radicals in tumor tissue and the possibility of their experimental influencing by means of antioxidants justifies the search for new pharmacological groups of tumor inhibiting agents. The authors synthesized a sterically inhibited, heterocyclic, bifunctional, non-toxic radical binding antioxidant of secondary amine type. The structural change is interpreted with the possibility of recombination characteristic for secondary amine groups and the double chain closing effect. The conjugation effect secures mobility of the hydrogen atom. The compound contains 10 to 12 per cent dimer-trimer of higher biological activity than monomers, due to higher molecular weight. An additional pharmacodynamic advantage compared to hitherto known antioxidants consists in its lower vapour volutility and the biradicality.
肿瘤组织中自由基的证据以及通过抗氧化剂对其进行实验性影响的可能性,为寻找新型肿瘤抑制药物类别提供了依据。作者合成了一种空间位阻型、杂环、双功能、无毒的仲胺型自由基结合抗氧化剂。结构变化被解释为仲胺基团的重组特性和双链封闭效应的可能性。共轭效应确保了氢原子的移动性。由于分子量较高,该化合物含有10%至12%的二聚体-三聚体,其生物活性高于单体。与迄今已知的抗氧化剂相比,其额外的药效学优势在于较低的蒸汽挥发性和双自由基性。