2. Academic Validation
  3. Design, synthesis and biological evaluations of novel pyridone-thiazole hybrid molecules as antitumor agents

Design, synthesis and biological evaluations of novel pyridone-thiazole hybrid molecules as antitumor agents

  • Eur J Med Chem. 2018 Feb 10:145:35-40. doi: 10.1016/j.ejmech.2017.12.038.
Wenlin Xie 1,  Yiqiang Wu 2,  Jingai Zhang 2,  Qihong Mei 2,  Yahan Zhang 2,  Ning Zhu 2,  Renzhi Liu 2,  Huilin Zhang 2
Affiliations

Affiliations

  • 1 School of Chemistry and Chemical Engineering, Hunan University of Science and Technology, Xiangtan 411201, China; Key Laboratory of Theoretical Organic Chemistry and Function Molecule of Ministry of Education, Hunan University of Science and Technology, Xiangtan 411201, China; Hunan Provincal Key Laboratory of Controllable Preparation and Functional Application of Fine Polymers, Xiangtan 411201, China. Electronic address: xwl2000zsu@163.com.
  • 2 School of Chemistry and Chemical Engineering, Hunan University of Science and Technology, Xiangtan 411201, China.
PMID: 29316536 DOI: 10.1016/j.ejmech.2017.12.038
Abstract

A hybrid pharmacophore approach was adopted to design and synthesize new series of pyridone-thiazole hybrid compounds. The structures of the compounds were established by IR, 1H NMR, 13C NMR, and HRMS. All the newly prepared compounds (3a-3m) were in vitro evaluated for their antiproliferative activity against three human Cancer cell lines, namely Colon Cancer (HCT-116), gastric carcinoma (MGC803) and hepatocellular Cancer (Huh7). Bioassay results demonstrated that most of the tested compounds showed potent anti-tumor activities against various Cancer cells in vitro, and some compounds exhibited stronger effects than positive control 5-Fluorouracil (5-FU). Compound 3b showed the best anti-tumor activity with IC50 values of 8.17 μM and 3.15 μM against HCT116 and MGC803 cell lines, respectively, which was 1.4-8.1 times more potent than 5-Fluorouracil (IC50 = 11.29 μM and 25.54 μM against HCT116 and MGC803 respectively). These findings suggest that compound 3b may have potential to be developed as a promising lead for the design of novel Anticancer small-molecule drugs.

Keywords

Antitumor activity; Hybrids; Pyridone; Synthesis; Thiazole.

Figures