Antiproliferation, 3D-multicellular spheroid and VEGFR-2 inhibitory properties of spiroindolin-2-ones with phosphonate function.

ABSTRACT: 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, t

SUBMITTER: Hassan SM 

PROVIDER: S-EPMC12504763 | biostudies-literature | 2025 Oct

REPOSITORIES: biostudies-literature