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, Seref Demirayak.

Journal Name: Letters in Drug Design & Discovery

Volume 16 , Issue 2 , 2019

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Graphical 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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Article Details

Year: 2019
Page: [111 - 118]
Pages: 8
DOI: 10.2174/1570180815666180606081042
Price: $58

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