title: 5-Benzylidene-2,4-thiazolidenedione derivatives: Design, synthesis and evaluation as inhibitors of angiogenesis targeting VEGR-2.
abstract: 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.
authors.affiliation: Department of Pharmaceutical Chemistry, Bharati Vidyapeeth's College of Pharmacy, C.B.D Belapur, Navi Mumbai 400614, Maharashtra, India.
authors.forename: Umesh
authors.initials: U
authors.lastname: Bhanushali
authors.affiliation: Vascular Biology Lab, AU KBC Research Center, MIT Campus, Chromepet, Chennai 600044, Tamil Nadu, India.
authors.forename: Saranya
authors.initials: S
authors.lastname: Rajendran
authors.affiliation: Dr. Reddy's Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500046, Andhra Pradesh, India.
authors.forename: Keerthana
authors.initials: K
authors.lastname: Sarma
authors.affiliation: Dr. Reddy's Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500046, Andhra Pradesh, India.
authors.forename: Pushkar
authors.initials: P
authors.lastname: Kulkarni
authors.affiliation: Dr. Reddy's Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500046, Andhra Pradesh, India.
authors.forename: Kiranam
authors.initials: K
authors.lastname: Chatti
authors.affiliation: Vascular Biology Lab, AU KBC Research Center, MIT Campus, Chromepet, Chennai 600044, Tamil Nadu, India.
authors.forename: Suvro
authors.initials: S
authors.lastname: Chatterjee
authors.affiliation: Department of Pharmaceutical Chemistry, Bharati Vidyapeeth's College of Pharmacy, C.B.D Belapur, Navi Mumbai 400614, Maharashtra, India. Electronic address: ramaa.cs@bharatividyapeeth.edu.
authors.forename: C S
authors.initials: CS
authors.lastname: Ramaa
mesh_terms: D000818:Animals; D001597:Benzylidene Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D006801:Humans; D015394:Molecular Structure; D009389:Neovascularization, Pathologic / Q000188:drug therapy* / Q000473:pathology; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D040301:Vascular Endothelial Growth Factor Receptor-2 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D015027:Zebrafish
chemical_list: D001597:Benzylidene Compounds; D047428:Protein Kinase Inhibitors; D013844:Thiazoles; D040301:Vascular Endothelial Growth Factor Receptor-2
keywords: 5-Benzylidene-2,4-thiazolidinediones; CAM assay; Docking; VEGFR2; Zebrafish embryo