Manfredini S, Vicentini C B, Manfrini M, Bianchi N, Rutigliano C, Mischiati C, Gambari R
Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Italy.
Bioorg Med Chem. 2000 Sep;8(9):2343-6. doi: 10.1016/s0968-0896(00)00160-7.
In view of the continuous interest in new DNA cleaving compounds, both for the development of new therapeutic agents and for the possible use as reagents in nucleic acids research, a few pyrazolo[3,4-d][1,2,3]triazole derivatives have been obtained and investigated for their antiproliferative activity and capability to cleave DNA, after light-activation. A possible in situ activation, i.e. in neoplastic tissues, of less cytotoxic derivatives, may lead to potential antitumor compounds endowed with high therapeutic indexes.
鉴于人们对新型DNA切割化合物持续感兴趣，这既用于开发新型治疗药物，也可能用作核酸研究中的试剂，我们已获得了一些吡唑并[3,4-d][1,2,3]三唑衍生物，并对其光激活后的抗增殖活性和切割DNA的能力进行了研究。细胞毒性较小的衍生物可能在肿瘤组织中发生原位激活，从而产生具有高治疗指数的潜在抗肿瘤化合物。
