Utility of 3-Acetyl-6-bromo-2H-chromen-2-one for the Synthesis of New Heterocycles as Potential Antiproliferative AgentsReportar como inadecuado




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1

Department of Chemistry, Faculty of Science, Cairo University, Giza 12613, Egypt

2

Department of Chemistry, Faculty of Science, Beni-Suef University, Beni-Suef 62514, Egypt





*

Author to whom correspondence should be addressed.



Academic Editor: Richard A. Bunce

Abstract Coumarin derivatives containing pyrazolo1,5-apyrimidine, tetrazolo1,5-apyrimidine, imidazo1,2-apyrimidine, pyrazolo3,4-dpyrimidine, 1,3,4-thiadiazoles and thiazoles were synthesized from 6-bromo-3-3-dimethylaminoacryloyl-2H-chromen-2-one, methyl 2-1-6-bromo-2-oxo-2H-chromen-3-ylethylidenehydrazine carbodithioate, 2-1-6-bromo-2-oxo-2H-chromen-3-ylethylidene hydrazine carbothioamide and each of heterocyclic amine, hydrazonoyl chlorides and hydroximoyl chlorides. The structures of the newly synthesized compounds were elucidated on the basis of elemental analysis, spectral data, and alternative synthetic routes whenever possible. Moreover, selected newly synthesized products were evaluated for their antitumor activity against a liver carcinoma cancer cell line HEPG2-1. The results revealed that pyrazolo1,5-apyrimidine 7c, thiazole 23g and 1,3,4-thiadiazole 18a IC50 = 2.70 ± 0.28, 3.50 ± 0.23 and 4.90 ± 0.69 µM, respectively have promising antitumor activity against liver carcinoma HEPG2-1 while most of the tested compounds showed moderate activity. View Full-Text

Keywords: pyrazolo1,5-apyrimidine; tetrazolo1,5-apyrimidine; 1,3,4-thiadiazoles; thiazoles; hydrazonoyl halides; hydroximoyl chlorides; antitumor activity pyrazolo1,5-apyrimidine; tetrazolo1,5-apyrimidine; 1,3,4-thiadiazoles; thiazoles; hydrazonoyl halides; hydroximoyl chlorides; antitumor activity





Autor: Sobhi M. Gomha 1, Yasser H. Zaki 2 and Abdou O. Abdelhamid 1,*

Fuente: http://mdpi.com/



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