2. Academic Validation
  3. 5-(4-Hydroxyphenyl)-3H-1,2-dithiole-3-thione derivatives of brefeldin A: Design, synthesis and cytotoxicity in MDA-MB-231 human breast cancer cells

5-(4-Hydroxyphenyl)-3H-1,2-dithiole-3-thione derivatives of brefeldin A: Design, synthesis and cytotoxicity in MDA-MB-231 human breast cancer cells

  • Bioorg Med Chem. 2023 Jul 15:90:117380. doi: 10.1016/j.bmc.2023.117380.
Mingying Wang 1,  Baojia Sun 2,  Tao Ye 1,  Yanbing Wang 3,  Yonglian Hou 1,  Siyuan Wang 4,  Huaqi Pan 5,  Huiming Hua 6,  Dahong Li 7
Affiliations

Affiliations

  • 1 Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, and School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, 103, Wenhua Road, Shenyang 110016, PR China.
  • 2 Yantai Valiant Pharmaceutical Co. Ltd., 60, Taiyuan Road, Dajijia Industrial Park, YEDA Yantai, Shandong 264006, PR China.
  • 3 School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
  • 4 College of Pharmacy, Shenzhen Technology University, Shenzhen 518118, PR China.
  • 5 Institute of Applied Ecology, Chinese Academy of Sciences, Shenyang 110016, PR China.
  • 6 Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, and School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, 103, Wenhua Road, Shenyang 110016, PR China. Electronic address: huimhua@163.com.
  • 7 Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, and School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, 103, Wenhua Road, Shenyang 110016, PR China. Electronic address: lidahong0203@163.com.
PMID: 37329677 DOI: 10.1016/j.bmc.2023.117380
Abstract

27 novel 5-(4-hydroxyphenyl)-3H-1,2-dithiole-3-thione derivatives of brefeldin A were designed and synthesized to make them more conducive to the Cancer treatment. The antiproliferative activity of all the target compounds was tested against six human Cancer cell lines and one human normal cell line. Compound 10d exhibited nearly the most potent cytotoxicity with IC50 values of 0.58, 0.69, 1.82, 0.85, 0.75, 0.33 and 1.75 μM against A549, DU-145, A375, HeLa, HepG2, MDA-MB-231 and L-02 cell lines. Moreover, 10d inhibited metastasis and induced Apoptosis of MDA-MB-231 cells in a dose-dependent manner. The potent Anticancer effects of 10d were prompted based on the aforementioned results, the therapeutic potential of 10d for breast Cancer was worth further exploration.

Keywords

2-Dithiole-3-thione; 5-(4-Hydroxyphenyl)-3H-1; Apoptosis; Breast cancer; Brefeldin A; Metastasis.

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