Synthesis, Docking Study, and Biological Evaluation of 2-Phenylchroman-4-One Derivatives As Murine Double Minute 2 (Mdm2) Inhibitors

Synthesis, Docking Study, and Biological Evaluation of 2-Phenylchroman-4-One Derivatives As Murine Double Minute 2 (Mdm2) Inhibitors Publisher

Talebi M¹ ; Boumi S¹ ; Nezamtaheri MS² ; Sarmad Y¹ ; Hosseini FS¹ ; Delphi L³ ; Goliaei B² ; Amini M¹ ; Amanlou M^{1, 4}

Show Affiliations

1. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
2. Laboratory of Biophysics and Molecular Biology, Institute of Biochemistry and Biophysics (IBB), University of Tehran, Tehran, Iran
3. Animal Biology Department, Faculty of Biology, University College of Sciences, University of Tehran, Tehran, Iran
4. Experimental Medicine Research Center, Tehran University of Medical Sciences, Tehran, Iran

Source: ChemistrySelect Published:2023

Abstract

Inhibiting the interaction between the p53 tumor suppressor and its negative regulator murine double minute 2 (MDM2) is a promising therapeutic opportunity in cancer drug research. Herein, we describe the design, synthesis, and in vitro screening of phenyl chroman-based derivatives 7 a–l as MDM2 inhibitors. Among target compounds, 7 e, 7 h, and 7 j had considerable cytotoxicity activity at concentrations of 50 μM and 100 μM against MCF7 and HCT-116 cell lines. Designed compounds that demonstrated good toxicity, were selected for enzyme inhibition assay. The most potent MDM2 inhibitor in this series is compound 7 h, which showed a Ki value of 13.66 μM. Moreover, compound 7 h with acceptable safety profiles in normal cells was found the least effective compound against human umbilical vein endothelial cells (HUVECs). In addition, cell cycle analysis was also investigated for representative compound 7 h. Also, the docking study was done to predict the possible interaction between the synthesized compound and both MDM2 and murine double minute x (MDMX) proteins. Interestingly, the docking results were in good agreement with the experimental assay. © 2023 Wiley-VCH GmbH.

Style	Citing Format
MLA	Talebi M, et al.. "Synthesis, Docking Study, and Biological Evaluation of 2-Phenylchroman-4-One Derivatives As Murine Double Minute 2 (Mdm2) Inhibitors." ChemistrySelect, vol. 8, no. 3, 2023, pp. -.
APA	Talebi M, Boumi S, Nezamtaheri MS, Sarmad Y, Hosseini FS, Delphi L, Goliaei B, Amini M, Amanlou M (2023). Synthesis, Docking Study, and Biological Evaluation of 2-Phenylchroman-4-One Derivatives As Murine Double Minute 2 (Mdm2) Inhibitors. ChemistrySelect, 8(3), -.
Chicago	Talebi M, Boumi S, Nezamtaheri MS, Sarmad Y, Hosseini FS, Delphi L, Goliaei B, Amini M, Amanlou M. "Synthesis, Docking Study, and Biological Evaluation of 2-Phenylchroman-4-One Derivatives As Murine Double Minute 2 (Mdm2) Inhibitors." ChemistrySelect 8, no. 3 (2023): -.
Harvard	Talebi M et al. (2023) 'Synthesis, Docking Study, and Biological Evaluation of 2-Phenylchroman-4-One Derivatives As Murine Double Minute 2 (Mdm2) Inhibitors', ChemistrySelect, 8(3), pp. -.
Vancouver	Talebi M, Boumi S, Nezamtaheri MS, Sarmad Y, Hosseini FS, Delphi L, et al.. Synthesis, Docking Study, and Biological Evaluation of 2-Phenylchroman-4-One Derivatives As Murine Double Minute 2 (Mdm2) Inhibitors. ChemistrySelect. 2023;8(3):-.
BibTex	@article{ author = {Talebi M and Boumi S and Nezamtaheri MS and Sarmad Y and Hosseini FS and Delphi L and Goliaei B and Amini M and Amanlou M}, title = {Synthesis, Docking Study, and Biological Evaluation of 2-Phenylchroman-4-One Derivatives As Murine Double Minute 2 (Mdm2) Inhibitors}, journal = {ChemistrySelect}, volume = {8}, number = {3}, pages = {-}, year = {2023} }
RIS	TY - JOUR AU - Talebi M AU - Boumi S AU - Nezamtaheri MS AU - Sarmad Y AU - Hosseini FS AU - Delphi L AU - Goliaei B AU - Amini M AU - Amanlou M TI - Synthesis, Docking Study, and Biological Evaluation of 2-Phenylchroman-4-One Derivatives As Murine Double Minute 2 (Mdm2) Inhibitors JO - ChemistrySelect VL - 8 IS - 3 SP - EP - PY - 2023 ER -

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