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作为光可激活DNA切割剂的吡唑并三唑类化合物。

Pyrazolo-triazoles as light activable DNA cleaving agents.

作者信息

Manfredini S, Vicentini C B, Manfrini M, Bianchi N, Rutigliano C, Mischiati C, Gambari R

机构信息

Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Italy.

出版信息

Bioorg Med Chem. 2000 Sep;8(9):2343-6. doi: 10.1016/s0968-0896(00)00160-7.

Abstract

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.

摘要

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。

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