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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 and Radadiya, Ashish 2022. Novel dihydropyrimidinone derivatives as potential P-glycoprotein modulators. ACS Omega 7 (19) , pp. 16278-16287. 10.1021/acsomega.1c05839

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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.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Chemistry
Additional Information: CC-BY
Publisher: American Chemical Society
ISSN: 2470-1343
Funders: University Grants Commission, New Delhi, India
Date of First Compliant Deposit: 4 May 2022
Date of Acceptance: 15 April 2022
Last Modified: 30 Jun 2022 08:34

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