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新型吡唑并[5,1-c][1,2,4]苯并三嗪、吡唑并[5,1-c]吡啶并[4,3-e][1,2,4]三嗪及其开链类似物作为常氧和低氧条件下细胞毒性剂的合成。

Synthesis of new pyrazolo[5,1-c][1,2,4] benzotriazines, pyrazolo[5,1-c]pyrido[4,3-e][1,2,4] triazines and their open analogues as cytotoxic agents in normoxic and hypoxic conditions.

作者信息

Ciciani Giovanna, Coronnello Marcella, Guerrini Gabriella, Selleri Silvia, Cantore Miriam, Failli Paola, Mini Enrico, Costanzo Annarella

机构信息

Dipartimento di Scienze Farmaceutiche, Università degli Studi di Firenze, Via U. Schiff 6, 50019 Polo Scientifico, Sesto Fiorentino, Firenze, Italy.

出版信息

Bioorg Med Chem. 2008 Nov 1;16(21):9409-19. doi: 10.1016/j.bmc.2008.09.055. Epub 2008 Sep 26.

DOI:10.1016/j.bmc.2008.09.055
PMID:18845441
Abstract

The synthesis and antitumor activity in normoxic and hypoxic conditions of a series of pyrazolo[5,1-c][1,2,4]benzotriazine and its related analogues are reported. All compounds were tested on human colorectal adenocarcinoma cell line HCT-8 and for compounds 15 and 20, which show to have selective cytotoxicity in hypoxic and in normoxic conditions respectively, ROS production, cell cycle, and DNA fragmentation were measured. This preliminary study encouraged us to consider 15 and 20 as interesting leads for further optimization.

摘要

报道了一系列吡唑并[5,1-c][1,2,4]苯并三嗪及其相关类似物在常氧和低氧条件下的合成及抗肿瘤活性。所有化合物均在人结肠腺癌HCT-8细胞系上进行测试，对于分别在低氧和常氧条件下具有选择性细胞毒性的化合物15和20，测定了活性氧生成、细胞周期和DNA片段化情况。这项初步研究促使我们将化合物15和20视为进一步优化的有趣先导化合物。

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