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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.
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Details
1 National Research Centre, Department of Pesticide Chemistry, Giza, Egypt (GRID:grid.419725.c) (ISNI:0000 0001 2151 8157)
2 Augusta University, Department of Chemistry and Physics, Augusta, USA (GRID:grid.410427.4) (ISNI:0000 0001 2284 9329)
3 National Research Centre, Center of Scientific Excellence for Influenza Viruses, Giza, Egypt (GRID:grid.419725.c) (ISNI:0000 0001 2151 8157)
4 Cardiff University, School of Chemistry, Cardiff, UK (GRID:grid.5600.3) (ISNI:0000 0001 0807 5670)
5 National Research Centre, Drug Bioassay-Cell Culture Laboratory, Pharmacognosy Department, Giza, Egypt (GRID:grid.419725.c) (ISNI:0000 0001 2151 8157)
6 Cairo University, Department of Pharmacognosy, Faculty of Pharmacy, Cairo, Egypt (GRID:grid.7776.1) (ISNI:0000 0004 0639 9286)
7 National Research Centre, Department of Therapeutic Chemistry, Giza, Egypt (GRID:grid.419725.c) (ISNI:0000 0001 2151 8157)