title: Tetrahydroquinoline-derived macrocyclic toolbox: the discovery of antiangiogenesis agents in zebrafish assay.
abstract: A novel approach to incorporate the macrocyclic rings onto the privileged substructure, i.e., tetrahydroquinoline scaffold, is developed. The presence of an amino acid-derived moiety in the macrocyclic skeleton provides an opportunity to modulate the nature of the chiral side chain. Further, evaluation in a zebrafish screen identified three active small molecules (2.5b, 3.2d, and 4.2) as antiangiogenesis agents at 2.5 μM.
authors.affiliation: Dr. Reddy's Institute of Life Sciences, University of Hyderabad Campus , Gachibowli, Hyderabad 500 046, India.
authors.forename: Shiva Krishna
authors.initials: SK
authors.lastname: Reddy Guduru
authors.affiliation: Dr. Reddy's Institute of Life Sciences, University of Hyderabad Campus , Gachibowli, Hyderabad 500 046, India.
authors.forename: Srinivas
authors.initials: S
authors.lastname: Chamakuri
authors.affiliation: School of Life Sciences, Södertörns Högskola, Sweden.
authors.forename: Gayathri
authors.initials: G
authors.lastname: Chandrasekar
authors.affiliation: School of Life Sciences, Södertörns Högskola, Sweden ; Division of Molecular Neurobiology and Department of Medical Biochemistry and Biophysics, Karolinska Institutet , Sweden.
authors.forename: Satish Srinivas
authors.initials: SS
authors.lastname: Kitambi
authors.affiliation: Dr. Reddy's Institute of Life Sciences, University of Hyderabad Campus , Gachibowli, Hyderabad 500 046, India.
authors.forename: Prabhat
authors.initials: P
authors.lastname: Arya
keywords: Natural product-inspired compounds; antiangiogenesis agents; macrocyclic diversity; zebrafish screen