Synthesis and anticancer activity of [1, 2, 4] triazole [4, 3-b] [1, 2, 4, 5] tetrazine derivatives. (21st September 2022)

• Record Type: Journal Article
• Authors: Pei, Tianyun; Zhang, Xuanhe; Yang, Zhenzhen; Ke, Zhonglu; Shi, Qingsong; Mao, Qingqing; Gong, Shunze; Zeng, Hanwei; Xu, Feng; Xu, Defeng
• Is Part Of: Phosphorus, sulfur, and silicon and the related elements. Volume 197:Number 8(2022)
• Page Start: 819
• Page End: 824
• Publication Date: 2022-09-21
• Subjects: Triazole -- tetrazine -- synthesis -- antitumor activity; Sulfur compounds -- Periodicals; Organosulfur compounds -- Periodicals; Phosphorus compounds -- Periodicals; Organophosphorus compounds -- Periodicals; Silicon compounds -- Periodicals; Organosilicon compounds -- Periodicals; 546
• DOI: 10.1080/10426507.2022.2033743
• Languages: English
• ISSNs: 1042-6507

Abstract

Abstract: A series of [1, 2, 4] triazole [4, 3-b] [1, 2, 4, 5] tetrazine derivatives were synthesized, and they were screened for their anticancer activity against human lung cancer (A549), mouse normal hepatocytes (AML12), human colorectal adenocarcinoma (CaCo2), human gastric cancer (EGC), human hepatocellular carcinoma (HEPG2) and human colon carcinoma (HT-29) cell lines. Among them, compound 4g (8-((6-(3, 5-Dimethyl-1 H -pyrazol-1-yl)-[1, 2, 4] triazolo[4, 3-b][1, 2, 4, 5]tetrazin-3-ylthio)methyl)quinoline) performed well, and its IC50 value against human colon carcinoma (HT-29) cell was 12.69 ± 7.14 µM. Graphical Abstract: UF0001