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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. ORCID:, Shah, Anamik and Radadiya, Ashish ORCID: 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: 22 Dec 2023 02:06

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