Effect of a novel series of benzothiazolo-quinazolones on epidermal growth factor receptor (EGFR) and biological evaluations.
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.
Shukla
Gauri
G
Division of Cyclotron and Radiopharmaceutical Sciences, Institute of Nuclear Medicine and Allied Sciences, Brig. S. K. Mazumdar Road, Delhi, India.
Tiwari
Anjani K
AK
Singh
Vinay K
VK
Bajpai
Aruna
A
Chandra
Harish
H
Mishra
Anil K
AK
D000818:Animals; D052160:Benzothiazoles / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology*; D045744:Cell Line, Tumor; D066246:ErbB Receptors / Q000037:antagonists & inhibitors*; D006801:Humans; D020128:Inhibitory Concentration 50; D007553:Isotope Labeling; D051379:Mice; D008826:Microbial Sensitivity Tests; D011799:Quinazolines / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology*; D013667:Technetium / Q000378:metabolism
D052160:Benzothiazoles; D011799:Quinazolines; D013667:Technetium; D066246:ErbB Receptors