The development of novel chemotherapeutic agents is indispensable to improve cancer treatment. One of the conventional approaches toward the synthesis of anticancer agents is the design of a compound whose structure is similar to purines found in DNA. In this study, a series of novel artificial purine nucleosides bearing selenotetrazole pharmacophore, 4a–4h, were synthesized. In order to get preliminary information about their cytotoxic activities, the interaction of compounds with DNA was investigated by UV titration and agarose gel electrophoresis and transcription inhibition studies were performed. The cytotoxic effects of the compounds against B16 melanoma, OV90 ovarian cancer, JM1 lymphoma cell lines, and PHA-induced peripheral blood lymphocytes were also investigated. In cell assay studies, the effects of the compounds on synthesis and mitosis stage of cell cycle were compared by flow cytometry. Although none of the compounds synthesized interacted with DNA and exhibited transcription inhibition, all of them significantly inhibited DNA synthesis phase and showed cytotoxic activity on cancer and proliferating cells.

新型化学治疗剂的开发对于改善癌症治疗必不可少。合成抗癌剂的常规方法之一是设计结构类似于DNA中嘌呤的化合物。在这项研究中，一系列新型的人工嘌呤核苷带有硒代托拉唑药效团，4a – 4h，被合成。为了获得有关其细胞毒性活性的初步信息，通过紫外线滴定和琼脂糖凝胶电泳研究了化合物与DNA的相互作用，并进行了转录抑制研究。还研究了该化合物对B16黑色素瘤，OV90卵巢癌，JM1淋巴瘤细胞系和PHA诱导的外周血淋巴细胞的细胞毒性作用。在细胞测定研究中，通过流式细胞术比较了化合物对细胞周期合成和有丝分裂阶段的影响。尽管合成的化合物均未与DNA相互作用并表现出转录抑制作用，但它们均能显着抑制DNA合成阶段并显示出对癌症和增殖细胞的细胞毒活性。