A novel heterocyclic compound inhibits human breast tumor cells via ROS mediated apoptosis

Article type: Research Article

Authors: Huang, Xia-Qian^{a; 1} | Ye, Wen-Hui^{b; 1} | Wu, Na-Ping^a | Fang, Qi^{a; *}

Affiliations: [a] Breast Surgery, Changzhou First People’s Hospital, Changzhou, Jiangsu, China | [b] Emergency Surgery, Changzhou First People’s Hospital, Changzhou, Jiangsu, China

Correspondence: [*] Corresponding author: Qi Fang, Emergency Surgery, Changzhou First People’s Hospital, Changzhou, Jiangsu, China. E-mail: fqi721228@126.com.

Note: [1] Authors are contributed equally to this work.

Abstract: The new heterocyclic compound 2-((6-chloro-2-methylpyrimidin-4-yl)amino)-N-(2-chloro-6-methylphenyl) thiazole-5-carboxamide (1), designed using 2-chloro-N-(2-chloro-6-methylphenyl)thiazole-5-carboxamide (2) as start material, was successfully obtained via multistep synthesis route and finally characterized by IR (infrared radiation), 1H NMR (nuclear magnetic resonance), and single crystal X-ray crystallography. The inhibitory effect of compound 1 on human breast tumor cell line BS524 was further explored. The MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) and IC50 (half maximal inhibitory concentration) values suggested that compound 1 has significant anti-proliferation activity on BS524 cells and with low side effect. Then, serial experiments, such as the Annexin V-FITC/PI assay, TUNEL staining and autophagy detection revealed that compound 1 could inhibit cell proliferation via induce cells apoptosis, and the apoptosis is induced by (reactive oxygen species) ROS generation in BS524 cells.

Keywords: Heterocycles, breast tumor, apoptosis, autophagy, flow cytometer, ROS

DOI: 10.3233/MGC-210008

Journal: Main Group Chemistry, vol. 20, no. 1, pp. 49-58, 2021