Design and biological evaluation of novel hybrids of 1, 5-diarylpyrazole and Chrysin for selective COX-2 inhibition

Bioorganic & Medicinal Chemistry
Shen-Zhen RenHai-Liang Zhu

Abstract

The overexpress of COX-2 was clearly associated with carcinogenesis and COX-2 as a possible target has long been exploited for cancer therapy. In this work, we described the design and synthesis of a series of diarylpyrazole derivatives integrating with chrysin. Among them, compound e9 exhibited the most potent inhibitory activity against COX-2 and antiproliferative activity against Hela cells with IC50 value of 1.12 μM. Further investigation revealed that e9 could induce apoptosis of Hela cells by mitochondrial depolarization and block the G1 phase of cell cycle in a dose-dependent manner. Besides, molecular docking simulation results was further confirmed that e9 could bind well with COX-2. In summary, compound e9 may be promising candidates for cancer therapy.

Citations

May 28, 2019·Expert Opinion on Therapeutic Patents·Sayyed Mohammad Ismail Mahboubi Rabbani, Afshin Zarghi
Dec 21, 2019·Journal of Enzyme Inhibition and Medicinal Chemistry·Youri OhJung-Mi Hah
Oct 1, 2020·Biomolecules·Ebrahim Rahmani MoghadamAlan Prem Kumar
Apr 2, 2021·Life Sciences·Hamid Reza SameniAhmad Reza Bandegi
Jun 3, 2021·Journal of Materials Chemistry. B, Materials for Biology and Medicine·Shen-Zhen RenHai-Liang Zhu

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