...
首页> 外文期刊>New Journal of Chemistry >Synthesis, characterization, and antiproliferative and apoptosis inducing effects of novel s-triazine derivatives
【24h】

Synthesis, characterization, and antiproliferative and apoptosis inducing effects of novel s-triazine derivatives

机译:新型S-三嗪衍生物的合成,表征和抗增殖和凋亡诱导诱导效应

获取原文
获取原文并翻译 | 示例
           

摘要

In an attempt to design and synthesize a new class of antitumor agents, a mild and eco-friendly protocol for nucleophilic substitution using an s-triazine scaffold, via amine and Schiff base derivatives, has been developed. In order to obtain antitumor activity, all synthesized compounds were screened in vitro for their cytotoxicity against human fibrosarcoma tumor cells (HT-1080) and a cervical cancer cell line (HeLa), for their ability to inhibit the growth of cancer cells. The selected s-triazine analogs (5c, 5d, and 6c) have been preliminarily studied for their reactive oxygen species (ROS) properties, mitochondrial membrane potential (MMP) and apoptosis (AO/EtBr) activity against the HT-1080 cancer cell line. The in vitro anticancer activity analysis has revealed that the synthesized compounds have good/moderate inhibitory activity against the tested cell lines compared to the standard drug. The theoretical study results also provide evidence that the s-triazines scaffolds have been successfully identified as superior p53-MDM2 inhibitors through structure-based design.
机译:在尝试设计和合成新类抗肿瘤剂,已经开发出使用S-Tri嗪支架,通过胺和Schiff基础衍生物进行轻度和生态友好的亲密性方案。为了获得抗肿瘤活性,将所有合成的化合物在体外筛选它们对人类纤维瘤肿瘤细胞(HT-1080)和宫颈癌细胞系(HELA)的细胞毒性,以抑制癌细胞生长的能力。已经预先研究了所选的S-三嗪类似物(5C,5D和6C),其对HT-1080癌细胞系的反应性氧物质(ROS)性质,线粒体膜电位(MMP)和凋亡(AO / ETBR)活性进行了预先研究。体外抗癌活性分析表明,与标准药物相比,合成化合物对测试细胞系具有良好/中度抑制活性。理论研究结果还提供了通过基于结构的设计成功被成功鉴定为优质P53-MDM2抑制剂的证据表明的证据表明,通过基于结构的设计成功地鉴定为优质的P53-MDM2抑制剂。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号