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Letters in Drug Design & Discovery

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ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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Research Article

Synthesis and Anticancer Activity of Some 1H-inden-1-one Substituted (Heteroaryl)Acetamide Derivatives

Author(s): Ahmet Cagri Karaburun, Nalan Gundogdu-Karaburun*, Leyla Yurttas, Ismail Kayagil and Seref Demirayak

Volume 16, Issue 2, 2019

Page: [111 - 118] Pages: 8

DOI: 10.2174/1570180815666180606081042

Price: $65

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.

Keywords: Anticancer activity, aurone analogue, benzothiazoleacetamide, 2, 3-dihydro-1H-inden-1-one, thiazoleacetamide, leukaemia.

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