Literature DB >> 24530491

Isothiocoumarin-3-carboxylic acid derivatives: synthesis, anticancer and antitrypanosomal activity evaluation.

Danylo Kaminskyy1, Anna Kryshchyshyn1, Ihor Nektegayev1, Olexandr Vasylenko2, Philippe Grellier3, Roman Lesyk4.   

Abstract

A series of new isothiocoumarin-3-carboxylic acids derivatives had been obtained based on the 5-arylidenerhodanines hydrolysis. Anticancer activity screening allowed identification of 7,8-dimethoxy-1-oxo-1H-isothiochromene-3-carboxylic acid (4-phenylthiazol-2-yl)-amide (30) with the highest level of antimitotic activity (GI50NCI-H322M/NSC Lung Cancer = 1.28 μM). Evaluation of the antitrypanosomal activity against Trypanosoma brucei brucei showed that investigated compounds did not exhibit significant antiparasitic effects. Additionally, the most pharmacologically attractive compounds were non-toxic and well tolerated by the experimental animals.
Copyright © 2014 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  5-Ylidenerhodanines; Anticancer activity; Antitrypanosomal activity; Isothiocoumarins; Synthesis

Mesh：

Substances：

Year:  2014        PMID： 24530491     DOI： 10.1016/j.ejmech.2014.01.028

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


  5 in total

1.  Hetero-Diels-Alder reactions of hetaryl and aryl thioketones with acetylenic dienophiles.

Authors:  Grzegorz Mlostoń; Paulina Grzelak; Maciej Mikina; Anthony Linden; Heinz Heimgartner
Journal:  Beilstein J Org Chem       Date:  2015-04-28       Impact factor: 2.883

2.  A facile synthesis and anticancer activity of some novel thiazoles carrying 1,3,4-thiadiazole moiety.

Authors:  Sobhi M Gomha; Nabila A Kheder; Mohamad R Abdelaziz; Yahia N Mabkhot; Ahmad M Alhajoj
Journal:  Chem Cent J       Date:  2017-03-21       Impact factor: 4.215

Review 3.  5-Ene-4-thiazolidinones - An efficient tool in medicinal chemistry.

Authors:  Danylo Kaminskyy; Anna Kryshchyshyn; Roman Lesyk
Journal:  Eur J Med Chem       Date:  2017-09-20       Impact factor: 6.514

4.  In vivo chemotherapeutic insight of a novel isocoumarin (3-hexyl-5,7-dimethoxy-isochromen-1-one): Genotoxicity, cell death induction, leukometry and phagocytic evaluation.

Authors:  Flávio Henrique Souza de Araújo; Débora Rojas de Figueiredo; Sarah Alves Auharek; João Renato Pesarini; Alisson Meza; Roberto da Silva Gomes; Antônio Carlos Duenhas Monreal; Andréia Conceição Milan Brochado Antoniolli-Silva; Dênis Pires de Lima; Candida Aparecida Leite Kassuya; Adilson Beatriz; Rodrigo Juliano Oliveira
Journal:  Genet Mol Biol       Date:  2017 Jul-Sep 01       Impact factor: 1.771

5.  Synthesis of novel thiazole, pyranothiazole, thiazolo[4,5-b]pyridines and thiazolo[5',4':5,6]pyrano[2,3-d]pyrimidine derivatives and incorporating isoindoline-1,3-dione group.

Authors:  Mona A Hosny; Yasser H Zaki; Wafaa A Mokbel; Abdou O Abdelhamid
Journal:  BMC Chem       Date:  2019-03-26
  5 in total

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