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: https://orcid.org/0000-0002-0375-0881, Shah, Anamik and Radadiya, Ashish ORCID: https://orcid.org/0000-0001-7348-1755 2022. Novel dihydropyrimidinone derivatives as potential P-glycoprotein modulators. ACS Omega 7 (19) , pp. 16278-16287. 10.1021/acsomega.1c05839

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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.

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
URI:	https://orca.cardiff.ac.uk/id/eprint/149517

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