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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 ?M.

SUBMITTER: Reddy Guduru SK 

PROVIDER: S-EPMC4027127 | biostudies-other | 2013 Jul

REPOSITORIES: biostudies-other

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Tetrahydroquinoline-derived macrocyclic toolbox: the discovery of antiangiogenesis agents in zebrafish assay.

Reddy Guduru Shiva Krishna SK   Chamakuri Srinivas S   Chandrasekar Gayathri G   Kitambi Satish Srinivas SS   Arya Prabhat P  

ACS medicinal chemistry letters 20130524 7


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. ...[more]

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