biostudies-literatureUnknown15(1)Hassan SMNational Research Centre EgyptSpiroindolin-2-ones with phosphonate function 17a‒t (20 analogs, 96‒72% yield) were generated by microwave synthetic methodology using azomethine cycloaddition of the appropriate 3,5-bis(ylidene)-4-piperidone-1-phosphonate 14a‒g. Single crystal X-ray analysis of 17d confirmed the structure. Promising 2D-monolayer antiproliferation properties (MTT assay) were observed for some of the synthesized agents with no harm to normal (RPE1) cell line. Compound 17h (R = 4-ClC₆H₄, R' = H; IC₅₀ = 3.08 μM; 6.6- and 3.1-fold the standard drugs, 5-fluorouracil and sunitinib, respectively) is the most distinguished agent against colon/HCT116 cell line. Compound 17f (R = 4-FC₆H₄, R' = Cl; IC₅₀ = 5.252 μM; 3.2-fold the activity of sunitinib, tScientific reports35018https://www.ebi.ac.uk/biostudies/studies/S-EPMC12504763biostudies-literatureAntiproliferation, 3D-multicellular spheroid and VEGFR-2 inhibitory properties of spiroindolin-2-ones with phosphonate function.PMC12504763Hassan SMFarid ANasr SKariuki BMSoliman AAFFayad WAbdelnaser APanda SSBekheit MSEl-Manawaty MAGirgis ASfalseAntiproliferation, 3D-multicellular spheroid and VEGFR-2 inhibitory properties of spiroindolin-2-ones with phosphonate function.Spiroindolin-2-ones with phosphonate function 17a‒t (20 analogs, 96‒72% yield) were generated by microwave synthetic methodology using azomethine cycloaddition of the appropriate 3,5-bis(ylidene)-4-piperidone-1-phosphonate 14a‒g. Single crystal X-ray analysis of 17d confirmed the structure. Promising 2D-monolayer antiproliferation properties (MTT assay) were observed for some of the synthesized agents with no harm to normal (RPE1) cell line. Compound 17h (R = 4-ClC₆H₄, R' = H; IC₅₀ = 3.08 μM; 6.6- and 3.1-fold the standard drugs, 5-fluorouracil and sunitinib, respectively) is the most distinguished agent against colon/HCT116 cell line. Compound 17f (R = 4-FC₆H₄, R' = Cl; IC₅₀ = 5.252 μM; 3.2-fold the activity of sunitinib, t2025-01-01T00:00:00Z2025 Oct2026-06-04T05:59:48.841Z2026-05-06T03:07:56.287ZS-EPMC125047634105750710.1038/s41598-025-20712-4