Design of New Benzohchromene Derivatives: Antitumor Activities and Structure-Activity Relationships of the 2,3-Positions and Fused Rings at the 2,3-PositionsReport as inadecuate


Design of New Benzohchromene Derivatives: Antitumor Activities and Structure-Activity Relationships of the 2,3-Positions and Fused Rings at the 2,3-Positions


Design of New Benzohchromene Derivatives: Antitumor Activities and Structure-Activity Relationships of the 2,3-Positions and Fused Rings at the 2,3-Positions - Download this document for free, or read online. Document in PDF available to download.

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Chemistry Department, Faculty of Science, Taibah University, 30002 Al-Madinah Al-Munawarah, Saudi Arabia

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Chemistry Department, Faculty of Scinece, King Khalid University, P.O. Box 9004, 61413 Abha, Saudi Arabia

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Chemistry Department, Faculty of Science, Al-Azhar University, Nasr City 11884, Cairo, Egypt





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Author to whom correspondence should be addressed.



Academic Editors: Philippe Belmont and Richard A. Bunce

Abstract A series of novel 4H-benzohchromenes 4, 6–11, 13, 14; 7H-benzohchromeno2,3-dpyrimidines 15–18, 20, and 14H-benzohchromeno3,2-e1,2,4triazolo1,5-cpyrimidine derivatives 19a–e, 24 was prepared. The structures of the synthesized compounds were characterized on the basis of their spectral data. Some of the target compounds were examined for their antiproliferative activity against three cell lines; breast carcinoma MCF-7, human colon carcinoma HCT-116 and hepatocellular carcinoma HepG-2. The cytotoxic behavior has been tested using MTT assay and the inhibitory activity was referenced to three standard anticancer drugs: vinblastine, colchicine and doxorubicin. The bioassays demonstrated that some of the new compounds exerted remarkable inhibitory effects as compared to the standard drugs on the growth of the three tested human tumor cell lines. The structure–activity relationships SAR study highlights that the antitumor activity of the target compounds was significantly affected by the lipophilicity of the substituent at 2- or 3- and fused rings at the 2,3-positions. View Full-Text

Keywords: benzochromene; benzochromenopyrimidine; benzochromenotriazolopyrimidine antitumor activities; SAR study benzochromene; benzochromenopyrimidine; benzochromenotriazolopyrimidine antitumor activities; SAR study





Author: Rawda M. Okasha 1,* , Fawzia F. Alblewi 1, Tarek H. Afifi 1, Arshi Naqvi 1, Ahmed M. Fouda 2, Al-Anood M. Al-Dies 2 and Ahmed M. El-Agrody 3

Source: http://mdpi.com/



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