Synthesis and Anticancer Activity of Some 1H-inden-1-one Substituted (Heteroaryl)Acetamide Derivatives
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Published:2018-11-29
Issue:2
Volume:16
Page:111-118
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ISSN:1570-1808
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Container-title:Letters in Drug Design & Discovery
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language:en
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Short-container-title:LDDD
Author:
Karaburun Ahmet Cagri1, Gundogdu-Karaburun Nalan1, Yurttas Leyla1, Kayagil Ismail2, Demirayak Seref3
Affiliation:
1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, 26470 Eskisehir, Turkey 2. Department of Chemistry, Faculty of Arts & Science, Mehmet Akif Ersoy University, 15030 Burdur, Turkey 3. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Medipol University, Istanbul, 34083, Turkey
Abstract
Background:
The synthesis of 2-[3/4-((6-substituted-1-oxo-2,3-dihydro-1H-inden-2-
ylidene)methyl)phenoxy]-N-(heteroaryl)acetamide derivatives and the investigation of their anticancer
activity were studied.
Methods:
2-(3/4-Hydroxybenzylidene)-6-substituted-2,3-dihydro-1H-inden-1-ones were reacted with
suitable 2-chloroacetamides to give 2-[3/4-((6-substituted-1-oxo-2,3-dihydro-1H-inden-2-ylidene)
methyl)phenoxy]-N-(heteroaryl)acetamide derivatives.
Results:
The structure elucidation of the newly synthesised 16 compounds was performed by IR,
1H-NMR, mass spectroscopic data and elemental analyses. The anticancer screening was carried
out in National Cancer Institute (NCI), USA.
Conclusion:
Compound 3e (2-(3-((6-chloro-1-oxo-2,3-dihydro-1H-inden-2-ylidene)methyl)phenoxy)-
N-(thiazol-2-yl)acetamide), exhibited highest growth inhibition against the leukaemia (61.47%),
non-small cell lung cancer (79.31%) and breast cancer (62.82%) cell lines.
Funder
Anadolu University, Turkey
Publisher
Bentham Science Publishers Ltd.
Subject
Drug Discovery,Pharmaceutical Science,Molecular Medicine
Reference30 articles.
1. Modranka J, Albrecht A, Jakubowski R, Krawczyk H, Rózalski M, Krajewska U, Janecka A, Wyrebska A, Rózalska B, Janecki T. Bioorg Med Chem Lett, Synthesis and biological evaluation of a-methylidene-d-lactones with 3,4-dihydrocoumarin skeleton.,, 2012, 20,, 5017-5026, 2. Keri RS, Budagumpi S, Pai RK, Balakrishna RG. Eur J Med Chem, Chromones as a privileged scaffold in drug discovery: A review.,, 2014, 78,, 340-374, 3. Emami S, Ghanbarimasir Z. Eur J Med Chem, Recent advances of chroman-4-one derivatives: Synthetic approaches and bioactivities.,, 2015, 26,, 539-563, 4. Seifert T, Malo M, Kokkola T, Engen K, Fridén-Saxin M, Wallén EAA, Kakkonen LM, Jarho EM, Luthman K. J Med Chem, Chroman-4-one- and chromone-based sirtuin 2 inhibitors with antiproliferative properties in cancer cells.,, 2014, 57,, 9870-9888, 5. Alizadeh BH, Saeedi M, Dehghan G, Foroumadi A, Shafiee A. J Iran Chem Soc, Synthesis of some novel pyrano [2,3-f]chromenone derivatives.,, 2015, 12,, 605-612,
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