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Effect of a Novel Series of Benzothiazolo‐Quinazolones on Epidermal Growth Factor Receptor (EGFR) and Biological Evaluations
Author(s) -
Shukla Gauri,
Tiwari Anjani K.,
Singh Vinay K.,
Bajpai Aruna,
Chandra Harish,
Mishra Anil K.
Publication year - 2008
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/j.1747-0285.2008.00724.x
Subject(s) - chemistry , acetic acid , epidermal growth factor receptor , in vivo , epidermal growth factor , combinatorial chemistry , biochemistry , receptor , biology , microbiology and biotechnology
A newly designed benzothiazolo‐quinazolone series was synthesized by an aromatic amine and potassium thiocyanate in the presence of bromine in glacial acetic acid, and the final product was obtained by subsequent reaction with 5‐arylamido/imidoalkyl‐2‐chlorobenzoic acid in the presence of potassium carbonate and further cyclization with sulphuric acid. A preliminary radiolabelling study with technetium shows a promising potential for further in vivo evaluation. Anti‐bacterial, anti‐viral and anti‐tumor activities were evaluated for biological properties. Lead compounds are able to block epidermal growth factor receptor (EGFR) in human breast adenocarcinoma cell line, MCF‐7.