Medicinal Chemistry Research

, Volume 26, Issue 10, pp 2583–2591 | Cite as

Synthesis and biological evaluation of novel N-(5-phenyl-1H-pyrazol-3-yl)benzenesulfonamide derivatives as potential BRAFV600E inhibitors

  • Zhen-Hua Gong
  • Jian Yao
  • Jian-Feng Ji
  • Jun Yang
  • Tie Xiang
  • Chang-Kai Zhou
Original Research
  • 63 Downloads

Abstract

A series of novel N-(5-phenyl-1H-pyrazol-3-yl)benzenesulfonamide derivatives (5a5l) were synthesized and developed as potential BRAFV600E inhibitors. Among them, compound 5l exhibited the most potent inhibitory activity with an IC50 value of 0.18 μM for BRAFV600E. Antiproliferative assay results indicated that compound 5l have higher antiproliferative activity against WM266.4 and A375 in vitro with IC50 value of 1.58 and 2.04 μM, respectively, which were comparable with the positive control vemurafenib. Molecular docking of 5l into the BRAFV600E active site was performed to determine the probable binding mode.

Keywords

BRAFV600E inhibitor Pyrazole Molecular docking Antiproliferative 

Notes

Acknowledgements

The authors are very much grateful to Nantong University, for providing laboratory facility.

Compliance with ethical standards

Conflict of interest

The authors declare that they have no competing interests.

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Copyright information

© Springer Science+Business Media, LLC 2017

Authors and Affiliations

  • Zhen-Hua Gong
    • 1
  • Jian Yao
    • 1
  • Jian-Feng Ji
    • 1
  • Jun Yang
    • 1
  • Tie Xiang
    • 1
  • Chang-Kai Zhou
    • 1
  1. 1.Department of Burn and Plastic SurgeryThe First People Hospital of NantongNantongChina

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