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Development of spiro-3-indolin-2-one containing compounds of antiproliferative and anti-SARS-CoV-2 properties

Fawazy, Nehmedo G., Panda, Siva S., Mostafa, Ahmed, Kariuki, Benson M. ORCID:, Bekheit, Mohamed S., Moatasim, Yassmin, Kutkat, Omnia, Fayad, Walid, El-Manawaty, May A., Soliman, Ahmed A. F., El-Shiekh, Riham A., Srour, Aladdin M., Barghash, Reham F. and Girgis, Adel S. 2022. Development of spiro-3-indolin-2-one containing compounds of antiproliferative and anti-SARS-CoV-2 properties. Scientific Reports 12 (1) , 13880. 10.1038/s41598-022-17883-9

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Abstract: A series of 1″-(alkylsulfonyl)-dispiro[indoline-3,2′-pyrrolidine-3′,3″-piperidine]-2,4″-diones 6a‒o has been synthesized through regioselective multi-component azomethine dipolar cycloaddition reaction of 1-(alkylsulfonyl)-3,5-bis(ylidene)-piperidin-4-ones 3a‒h. X-ray diffraction studies (6b‒d, h) confirmed the structures. The majority of the synthesized analogs reveal promising antiproliferation properties against a variety of human cancer cell lines (MCF7, HCT116, A431 and PaCa2) with good selectivity index towards normal cell (RPE1). Some of the synthesized agents exhibit potent inhibitory properties against the tested cell lines with higher efficacies than the standard references (sunitinib and 5-fluorouracil). Compound 6m is the most potent. Multi-targeted inhibitory properties against EGFR and VEGFR-2 have been observed for the synthesized agents. Flow cytometry supports the antiproliferation properties and shows the tested agents as apoptosis and necrosis forming. Vero cell viral infection model demonstrates the anti-SARS-CoV-2 properties of the synthesized agents. Compound 6f is the most promising (about 3.3 and 4.8 times the potency of the standard references, chloroquine and hydroxychloroquine). QSAR models explain and support the observed biological properties.

Item Type: Article
Date Type: Published Online
Status: Published
Schools: Chemistry
Additional Information: License information from Publisher: LICENSE 1: URL:, Type: open-access
Publisher: Nature Research
ISSN: 2045-2322
Date of First Compliant Deposit: 18 August 2022
Date of Acceptance: 2 August 2022
Last Modified: 10 Nov 2022 11:50

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