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Molecules 2017, 22(3), 479; doi:10.3390/molecules22030479

Design of New Benzo[h]chromene Derivatives: Antitumor Activities and Structure-Activity Relationships of the 2,3-Positions and Fused Rings at the 2,3-Positions

Chemistry Department, Faculty of Science, Taibah University, 30002 Al-Madinah Al-Munawarah, Saudi Arabia
Chemistry Department, Faculty of Scinece, King Khalid University, P.O. Box 9004, 61413 Abha, Saudi Arabia
Chemistry Department, Faculty of Science, Al-Azhar University, Nasr City 11884, Cairo, Egypt
Author to whom correspondence should be addressed.
Academic Editors: Philippe Belmont and Richard A. Bunce
Received: 27 January 2017 / Revised: 11 March 2017 / Accepted: 13 March 2017 / Published: 18 March 2017
(This article belongs to the Collection Heterocyclic Compounds)
View Full-Text   |   Download PDF [2384 KB, uploaded 18 March 2017]   |  


A series of novel 4H-benzo[h]chromenes 4, 611, 13, 14; 7H-benzo[h]chromeno[2,3-d]pyrimidines 1518, 20, and 14H-benzo[h]chromeno[3,2-e][1,2,4]triazolo[1,5-c]pyrimidine derivatives 19ae, 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

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Okasha, R.M.; Alblewi, F.F.; Afifi, T.H.; Naqvi, A.; Fouda, A.M.; Al-Dies, A.-A.M.; El-Agrody, A.M. Design of New Benzo[h]chromene Derivatives: Antitumor Activities and Structure-Activity Relationships of the 2,3-Positions and Fused Rings at the 2,3-Positions. Molecules 2017, 22, 479.

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