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Molecules 2018, 23(3), 693; https://doi.org/10.3390/molecules23030693

Synthesis of Some Novel Fused Pyrimido[4″,5″:5′,6′]-[1,2,4]triazino[3′,4′:3,4] [1,2,4]triazino[5,6-b]indoles with Expected Anticancer Activity

1
Chemistry Department, Faculty of Science, Taif University, Taif 21974, Saudi Arabia
2
Department of Basic Science, Faculty of Industrial Education, Helwan University, Cairo 11795, Egypt
3
Chemistry Department, Faculty of Science, Zagazig University, Zagazig 44511, Egypt
*
Author to whom correspondence should be addressed.
Received: 25 February 2018 / Revised: 13 March 2018 / Accepted: 16 March 2018 / Published: 19 March 2018
(This article belongs to the Collection Heterocyclic Compounds)
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Abstract

Our current goal is the synthesis of polyheterocyclic compounds starting from 3-amino-[1,2,4]triazino[5,6-b]indole 1 and studying their anticancer activity to determine whether increasing of the size of the molecules increases the anticancer activity or not. 1-Amino[1,2,4]triazino[3′,4′:3,4]-[1,2,4]triazino[5,6-b]indole-2-carbonitrile (4) was prepared by the diazotization of 3-amino[1,2,4]-triazino[5,6-b]indole 1 followed by coupling with malononitrile in basic medium then cyclization under reflux to get 4. Also, new fused pyrimido[4″,5″:5′,6′][1,2,4]triazino-[3′,4′:3,4][1,2,4]triazino[5,6-b]indole derivative 6 was prepared and used to obtain polycyclic heterocyclic systems. Confirmation of the synthesized compounds’ structures was carried out using elemental analyses and spectral data (IR, 1H-NMR and 13C-NMR and mass spectra). The anticancer activity of some of the synthesized compounds was tested against HepG2, HCT-116 and MCF-7 cell lines. The anticancer screening results showed that some derivatives display good activity which was more potent than that of the reference drug used. Molecular docking was used to predict the binding between some of the synthesized compounds and the prostate cancer 2q7k hormone and breast ‎cancer 3hb5 receptors. View Full-Text
Keywords: triazino[5,6-b]indole; pyrimido[2′,1′:3,4]triazino[5,6-b]indole; anticancer activity; molecular docking triazino[5,6-b]indole; pyrimido[2′,1′:3,4]triazino[5,6-b]indole; anticancer activity; molecular docking
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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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Ali, R.S.; Saad, H.A. Synthesis of Some Novel Fused Pyrimido[4″,5″:5′,6′]-[1,2,4]triazino[3′,4′:3,4] [1,2,4]triazino[5,6-b]indoles with Expected Anticancer Activity. Molecules 2018, 23, 693.

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