Literature DB >> 24836070

Benzofuran derivatives as anticancer inhibitors of mTOR signaling.

Christophe Salomé1, Nigel Ribeiro1, Thierry Chavagnan1, Frédéric Thuaud1, Maria Serova2, Armand de Gramont2, Sandrine Faivre3, Eric Raymond3, Laurent Désaubry4.   

Abstract

A series of 32 derivatives and isosteres of the mTOR inhibitor 2 were synthesized and compared for their cytotoxicity in radioresistant SQ20B cancer cell line. Several of these compounds, in particular 30b, were significantly more cytotoxic than 2. Importantly, 30b was shown to block both mTORC1 and Akt signaling, suggesting insensitivity to the resistance associated to Akt overactivation observed with rapamycin derivatives currently used in clinic.
Copyright © 2014 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Benzofuran; Cancer; Cytotoxicity; Rapamycin; mTOR

Mesh：

Substances：

Year:  2014        PMID： 24836070     DOI： 10.1016/j.ejmech.2014.05.014

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


  6 in total

Review 1.  Structure-Activity Relationship of Benzofuran Derivatives with Potential Anticancer Activity.

Authors:  Joviana Farhat; Lara Alzyoud; Mohammad Alwahsh; Basem Al-Omari
Journal:  Cancers (Basel)       Date:  2022-04-28       Impact factor: 6.575

2.  Identification of 3-(piperazinylmethyl)benzofuran derivatives as novel type II CDK2 inhibitors: design, synthesis, biological evaluation, and in silico insights.

Authors:  Wagdy M Eldehna; Raed M Maklad; Hadia Almahli; Tarfah Al-Warhi; Eslam B Elkaeed; Mohammed A S Abourehab; Hatem A Abdel-Aziz; Ahmed M El Kerdawy
Journal:  J Enzyme Inhib Med Chem       Date:  2022-12       Impact factor: 5.756

3.  Chemical and structural studies provide a mechanistic basis for recognition of the MYC G-quadruplex.

Authors:  David R Calabrese; Xiang Chen; Elena C Leon; Snehal M Gaikwad; Zaw Phyo; William M Hewitt; Stephanie Alden; Thomas A Hilimire; Fahu He; Aleksandra M Michalowski; John K Simmons; Lindsey B Saunders; Shuling Zhang; Daniel Connors; Kylie J Walters; Beverly A Mock; John S Schneekloth
Journal:  Nat Commun       Date:  2018-10-12       Impact factor: 14.919

4.  Cyclopropylmethyl Protection of Phenols: Total Synthesis of the Resveratrol Dimers Anigopreissin A and Resveratrol-Piceatannol Hybrid.

Authors:  Arvind Kumar; Michael Saleeb; Dominik Werz; Mikael Elofsson
Journal:  ChemistryOpen       Date:  2018-11-05       Impact factor: 2.911

5.  Novel oxindole/benzofuran hybrids as potential dual CDK2/GSK-3β inhibitors targeting breast cancer: design, synthesis, biological evaluation, and in silico studies.

Authors:  Wagdy M Eldehna; Sara T Al-Rashood; Tarfah Al-Warhi; Razan O Eskandrani; Amal Alharbi; Ahmed M El Kerdawy
Journal:  J Enzyme Inhib Med Chem       Date:  2021-12       Impact factor: 5.051

6.  Synthesis of Elaborate Benzofuran-2-carboxamide Derivatives through a Combination of 8-Aminoquinoline Directed C-H Arylation and Transamidation Chemistry.

Authors:  Michael Oschmann; Linus Johansson Holm; Monireh Pourghasemi-Lati; Oscar Verho
Journal:  Molecules       Date:  2020-01-15       Impact factor: 4.411
  6 in total

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