Chemical synthesis, docking studies and biological effects of functionalized 1,3-diaryl-2-propen-1-ones on human colon cancer cells

  • Guo-Min Zhu Department of Surgery, The First Affiliated Hospital of Nanchang University, Nanchang 330006
  • Guo-Dong Huang Guo-Dong Huang, Department of Integrated Traditional Chinese and Western Medicine, The First Affiliated Hospital of Nanchang University, No. 17 Yongwai Street, Nanchang, Jiangxi 330006
Keywords: 1, 3-Diaryl-2-propen-1-ones, Anticancer agents, Indolyl chalcones, colon cancer

Abstract

A series of 1, 3-diaryl-2-propen-1-ones was synthesised in order to obtain a new type of anticancer drug, designed with hybrid features to inhibit colon cancer activated receptor. Based on computational modelling and docking studies, potential inhibitors were synthesised and their biological activity evaluated. The structures of newly synthesized compounds were confirmed by 1HNMR, 13CNMR and Mass spectrometry. All analogues were evaluated for in vitro cytotoxicity against human colon (caco-2) cancer cell lines. Compounds 1b, 1f-1h, and 2i showed significant cytotoxicity. Chalcones 1b, 1f and 1g were identified as the most potent and selective anticancer agents with IC50 values <1 µg/mL and 1.5 µg/mL, against caco-2 cell line, respectively. In conclusion, this finding confirms the suitability of indolyl chalcone analogues as candidates for further investigation towards the management of colon cancer related diseases.

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Published
2015-03-16
How to Cite
Zhu, G.-M., and G.-D. Huang. “Chemical Synthesis, Docking Studies and Biological Effects of Functionalized 1,3-Diaryl-2-Propen-1-Ones on Human Colon Cancer Cells”. Bangladesh Journal of Pharmacology, Vol. 10, no. 1, Mar. 2015, pp. 230-4, doi:10.3329/bjp.v10i1.21699.
Section
Research Articles