5-亚苄基-2,4-噻唑烷二酮衍生物：作为靶向VEGR-2的血管生成抑制剂的设计、合成与评估
5-Benzylidene-2,4-thiazolidenedione derivatives: Design, synthesis and evaluation as inhibitors of angiogenesis targeting VEGR-2.
作者信息
Bhanushali Umesh, Rajendran Saranya, Sarma Keerthana, Kulkarni Pushkar, Chatti Kiranam, Chatterjee Suvro, Ramaa C S
机构信息
Department of Pharmaceutical Chemistry, Bharati Vidyapeeth's College of Pharmacy, C.B.D Belapur, Navi Mumbai 400614, Maharashtra, India.
Vascular Biology Lab, AU KBC Research Center, MIT Campus, Chromepet, Chennai 600044, Tamil Nadu, India.
出版信息
Bioorg Chem. 2016 Aug;67:139-47. doi: 10.1016/j.bioorg.2016.06.006. Epub 2016 Jun 30.
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 0.5μM against VEGFR-2.
设计了一系列新型5-亚苄基-2,4-噻唑烷二酮作为靶向血管内皮生长因子受体-2（VEGFR-2）的血管生成抑制剂。在对接研究中，这些分子与VEGFR-2的结合方式与共结晶配体相似。然后通过光谱技术对化合物进行合成、纯化和表征。发现化合物3f和3i在该系列中活性最高，在鸡胚绒毛尿囊膜（CAM）和斑马鱼胚胎试验中均显示出良好的血管生成抑制作用。化合物3i对VEGFR-2的半数抑制浓度（IC50）也为0.5μM。
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