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Novel Dihydropyrimidinone Derivatives as Potential P-Glycoprotein Modulators.
Bijani, Sabera; Shaikh, Faraz; Mirza, Sheefa; Weng In Siu, Shirley; Jain, Nayan; Rawal, Rakesh; Richards, Nigel G J; Shah, Anamik; Radadiya, Ashish.
Affiliation
  • Bijani S; Center of Excellence, National Facility for Drug Discovery Complex, Department of Chemistry, Saurashtra University, Rajkot 360005, India.
  • Shaikh F; Department of Chemistry, Marwadi University, Rajkot 360003, India.
  • Mirza S; Center of Excellence, National Facility for Drug Discovery Complex, Department of Chemistry, Saurashtra University, Rajkot 360005, India.
  • Weng In Siu S; Department of Computer and Information Science, University of Macau, Macau 999078, China.
  • Jain N; The Gujarat Cancer & Research Institute, Ahmedabad 380009, India.
  • Rawal R; Department of Internal Medicine, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South Africa.
  • Richards NGJ; Department of Computer and Information Science, University of Macau, Macau 999078, China.
  • Shah A; Department of Life Sciences, School of Sciences, Gujarat University, Ahmedabad 380009, India.
  • Radadiya A; The Gujarat Cancer & Research Institute, Ahmedabad 380009, India.
ACS Omega ; 7(19): 16278-16287, 2022 May 17.
Article in En | MEDLINE | ID: mdl-35601326
ABSTRACT
P-glycoprotein (Pgp), an ATP binding cassette (ABC) transporter, is an ATP-dependent efflux pump responsible for cancer multidrug resistance. As part of efforts to identify human Pgp (hPgp) inhibitors, we prepared a series of novel triazole-conjugated dihydropyrimidinones using a synthetic approach that is well suited for obtaining compound libraries. Several of these dihydropyrimidinone derivatives modulate human P-glycoprotein (hPgp) activity with low micromolar EC50 values. Molecular docking studies suggest that these compounds bind to the M-site of the transporter.
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Full text: 1 Database: MEDLINE Language: En Year: 2022 Type: Article
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Full text: 1 Database: MEDLINE Language: En Year: 2022 Type: Article