Literature DB >> 26491980

Synthesis and anticancer activity of 6-heteroarylcoumarins.

Olexandr Galayev1, Yana Garazd1, Myroslav Garazd1, Roman Lesyk2.   

Abstract

A series of novel 7-hydroxy-8-methyl-coumarins with indole, pyrimidine, pyrazole, pyran, tetrazolo[1,5-a]pyrimidine, pyrimido[1,2-a]benzimidazol, 2-oxo-1,2-dihydropyridine and dihydropyrazolo[3,4-b]pyridine moieties at C6 position of heterocyclic core have been synthesized. Anticancer activity screening on NCI60 cell lines allowed identification of 6-(6-fluoro-1H-indol-2-yl)-7-hydroxy-4,8-dimethyl-2H-chromen-2-one (23) with the highest level of antimitotic activity with mean GI50/TGI values of 3.28/13.24 μM and certain sensitivity profile towards the Non-Small Cell Lung Cancer cell line НОР-92 (GI50/TGI/LC50 values 0.95/4.17/29.9 μM).
Copyright © 2015 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  6-Heteroarylcoumarins; Anticancer activity; Synthesis

Mesh:

Substances:

Year:  2015        PMID: 26491980     DOI: 10.1016/j.ejmech.2015.10.021

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  3 in total

1.  Synthesis and evaluation of anticancer activity of 6-pyrazolinylcoumarin derivatives.

Authors:  Yana Garazd; Myroslav Garazd; Roman Lesyk
Journal:  Saudi Pharm J       Date:  2016-06-03       Impact factor: 4.330

2.  Extending the Inhibition Profiles of Coumarin-Based Compounds Against Human Carbonic Anhydrases: Synthesis, Biological, and In Silico Evaluation.

Authors:  Victor Kartsev; Athina Geronikaki; Silvia Bua; Alessio Nocentini; Anthi Petrou; Boris Lichitsky; Mykhaylo Frasinyuk; Janis Leitans; Andris Kazaks; Kaspars Tars; Claudiu T Supuran
Journal:  Molecules       Date:  2019-10-04       Impact factor: 4.411

3.  A Coumarin-Based Analogue of Thiacetazone as Dual Covalent Inhibitor and Potential Fluorescent Label of HadA in Mycobacterium tuberculosis.

Authors:  Asma Farjallah; Laurent R Chiarelli; Martin Forbak; Giulia Degiacomi; Mathieu Danel; Fernanda Goncalves; Chantal Carayon; Cendrine Seguin; Marco Fumagalli; Monika Záhorszká; Elodie Vega; Souhir Abid; Anna Grzegorzewicz; Mary Jackson; Antonio Peixoto; Jana Korduláková; Maria Rosalia Pasca; Christian Lherbet; Stefan Chassaing
Journal:  ACS Infect Dis       Date:  2021-02-22       Impact factor: 5.084

  3 in total

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