Human T cell lymphotropic virus type 1 (HTLV-1) is a human retrovirus that infects approximately 10–20 million people worldwide and causes an aggressive neoplasia (adult T-cell leukemia/lymphoma - ATL). Therapeutic approaches for the treatment of ATL have variable effectiveness and poor prognosis, thus requiring strategies to identify novel compounds with activity on infected cells. In this sense, we initially screened a small series of 25 1,2,3-triazole derivatives to discover cell proliferation inhibitors and apoptosis inducers in HTLV-1-infected T-cell line (MT-2) for further assessment of their effect on viral tax activity through inducible-tax reporter cell line (Jurkat LTR-GFP). Eight promising compounds (02, 05, 06, 13, 15, 21, 22 and 25) with activity ≥70% were initially selected, based on a suitable cell-based assay using resazurin reduction method, and evaluated towards cell cycle, apoptosis and Tax/GFP expression analyses through flow cytometry. Compound 02 induced S phase cell cycle arrest and compounds 05, 06, 22 and 25 promoted apoptosis. Remarkably, compounds 22 and 25 also reduced GFP expression in an inducible-tax reporter cell, which suggests an effect on Tax viral protein. More importantly, compounds 02, 22 and 25 were not cytotoxic in human hepatoma cell line (Huh-7). Therefore, the discovery of 3 active and non-cytotoxic compounds against HTLV-1-infected cells can potentially contribute, as an initial promising strategy, to the development process of new drugs against ATL.

1型人类T细胞淋巴病毒（HTLV-1）是一种人类逆转录病毒，感染了全世界约10-20百万人，并引起侵袭性肿瘤（成人T细胞白血病/淋巴瘤-ATL）。治疗ATL的治疗方法疗效不一，预后差，因此需要策略来鉴定对感染细胞具有活性的新型化合物。从这个意义上讲，我们最初筛选了25个1,2,3-三唑衍生物的小系列，以发现HTLV-1感染的T细胞系（MT-2）中的细胞增殖抑制剂和凋亡诱导剂，以进一步评估其对TLV-1的作用。通过诱导税收报告细胞系（Jurkat LTR-GFP）进行病毒税收活动。八种有前途的化合物（02，05，06，13，15，21，22和25）具有活性的≥70％的最初选择的基础上，合适的基于细胞的刃天青使用还原法测定，并朝向细胞周期，细胞凋亡和税务/ GFP表达分析评价通过流式细胞仪。合成化合物02诱导的S期的细胞周期停滞和化合物05，06，22和25促进细胞凋亡。值得注意的是，化合物22和25也以诱导税的方式降低了GFP的表达报告细胞，提示对Tax病毒蛋白有影响。更重要的是，化合物02，22和25不是在人肝癌细胞系（的Huh-7）的细胞毒性。因此，发现3种针对HTLV-1感染细胞的活性和非细胞毒性化合物可能作为一种有前途的策略，为抗ATL新药的开发过程做出贡献。