5-Benzylidene-2,4-thiazolidenedione derivatives: Design, synthesis and evaluation as inhibitors of angiogenesis targeting VEGR-2

• Designing of novel inhibitor of VEGFR-2 as per the reported pharmacophore.
• These compounds were synthesized purified and was characterized by spectroscopic techniques.
• Compound were initially screen for the preliminary angiogenesis assay followed by the VEGFR-2 inhibition assay of the most active compound (3f, 3i).
• Compound 3i was found to be most active in the series with IC50 of 0.5 μm.

A series of novel 5-benzylidene-2,4-thiazolidinediones were designed as inhibitors of angiogenesis targeting VEGFR-2. In docking study, molecules showed similar way of binding with VEGFR-2 as that of the co-crystallized ligand. Compounds were then synthesized, purified and characterized by spectroscopic techniques. Compounds 3f and 3i were found to be most active in the series showing good inhibition of angiogenesis in both CAM and in zebrafish embryo assays. Compound 3i also exhibited IC50 of 0.5 μM against VEGFR-2.

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