NDLI: Synthesis, biological activity and docking study of some new isatin Schiff base derivatives

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Synthesis, biological activity and docking study of some new isatin Schiff base derivatives

Content Provider	Semantic Scholar
Author	Azizian, Javad Mohammadi, Mohammad Kazem Firuzi, Omidreza Razzaghi-Asl, Nima Miri, Ramin
Copyright Year	2011
Abstract	A set of novel Schiff bases of isatin were synthesized and characterized by reaction of isatin with various aromatic or heterocyclic primary amines. Cytotoxic activities for some of the synthesized compounds were evaluated by MTT assay in three human cancer cell lines (HeLa, LS180 and Raji). Half of the tested compounds showed good cytotoxicity in HeLa cells. 3-(2-(4-nitrophenyl) hydrazono) indolin-2-one was found to be the most potent molecule among the studied isatin derivatives. Docking studies of 3-substituted indolin-2-one scaffolds on vascular endothelial growth factor receptor 2 (VEGFR-2) involved in cell proliferation and angiogenesis was performed. 3-(naphthalen-1-ylimino) indolin-2-one and 3-(2-(4-nitrophenyl) hydrazono) indolin-2-one exhibited higher docking binding energies with receptor. For 3-(2-(4-nitrophenyl) hydrazono) indolin-2-one, H-bond interaction with Cys917 residue of target active site was in common with reported crystallographic benzoimidazole derivative (PDB code: 2OH4). New key H-bonds involving Glu915, Asn921, and Arg1049 residues in VEGFR-2 active site could be detected for 3-(2-(4-nitrophenyl) hydrazono) indolin-2-one. Extended lipophilic rings containing H-bond acceptors on the 3 position of indoline scaffold seemed to be important factors in developing potent VEGFR-2 inhibitors virtually. Based on the ligand efficiency indices, some isoxazole or thiazole substituted isatin derivatives may be regarded as efficient candidates for further molecular developments of anticancer agents.
Starting Page	3730
Ending Page	3740
Page Count	11
File Format	PDF HTM / HTML
DOI	10.1007/s00044-011-9896-6
Volume Number	21
Alternate Webpage(s)	https://eprints.arums.ac.ir/5388/7/Synthesis.pdf
Journal	Medicinal Chemistry Research
Language	English
Access Restriction	Open
Content Type	Text
Resource Type	Article

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