NDLI: Synthesis, structure activity relationships and biological activity evaluation of novel spirocyclic thiazolidin-4-ones as potential anti-breast cancer and epidermal growth factor receptor inhibitors.

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Synthesis, structure activity relationships and biological activity evaluation of novel spirocyclic thiazolidin-4-ones as potential anti-breast cancer and epidermal growth factor receptor inhibitors.

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Synthesis, structure activity relationships and biological activity evaluation of novel spirocyclic thiazolidin-4-ones as potential anti-breast cancer and epidermal growth factor receptor inhibitors.

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Fleita, D. H. Sakka, O. K. Mohareb, R. M.
Description	Country affiliation: Egypt Author Affiliation: Fleita DH ( Department of Chemistry, American University in Cairo, New Cairo, Egypt.); Sakka OK ( Department of Chemistry, American University in Cairo, New Cairo, Egypt.); Mohareb RM ( Department of Chemistry, Faculty of Science, Cairo University, Giza, Egypt.)
Abstract	A series of triazaspiro[4.5]dec-8-ene benzylidine derivatives containing thiazolidinone ring system (6-18) have been designed, synthesized and their biological activities evaluated as potential epidermal growth factor receptor inhibitors. Among them, 9-amino-2-(4-nitrobenzylidene)-3-oxo-4-phenyl-7-thioxo-1-thia-4,6,8-triazaspiro[4.5]dec-8-ene-10-carbonitrile (18) displayed the most potent inhibitory activity (IC50=6.355 µM). Antiproliferative assay results indicated that compound 18 exhibited moderate antiproliferative activity against MCF-7 cell line in vitro; with GI50 value of 30.6 µM. In addition, compounds 7 and 15 displayed the highest antiproliferative activity at a common GI50 value of 10.8 µM. Docking simulation was performed to determine the probable binding model and to pursuit information regarding the activity of compound 18. Based on the preliminary results, compound 18 could be used as an attractive building block for designing potential epidermal growth factor receptor inhibitors.
File Format	HTM / HTML
ISSN	21949379
Issue Number	1
Volume Number	64
e-ISSN	21949387
Journal	Drug Research
Language	English
Publisher	Thieme
Publisher Date	2014-01-01
Publisher Place	Germany
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Discipline Pharmacology Antineoplastic Agents Chemical Synthesis Pharmacology Breast Neoplasms Drug Therapy Receptor, Epidermal Growth Factor Antagonists & Inhibitors Thiazolidines Cell Line, Tumor Cell Proliferation Drug Effects Dimethyl Sulfoxide Female Humans Indicators And Reagents Magnetic Resonance Spectroscopy Models, Molecular Protein Kinase Inhibitors Quantum Theory Spectrophotometry, Infrared Structure-activity Relationship Journal Article Research Support, Non-u.s. Gov't
Content Type	Text
Resource Type	Article
Subject	Medicine Drug Discovery

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