Literature DB >> 22119128

Design, synthesis and in vitro antitumour activity of new heteroaryl ethylenes.

Cosimo G Fortuna1, Vincenza Barresi, Carmela Bonaccorso, Giuseppe Consiglio, Salvatore Failla, Angela Trovato-Salinaro, Giuseppe Musumarra.   

Abstract

Almond and VolSurf + modelling procedures allowed the structural design of new di- and mono-heteroaryl-ethylenes. The structural modifications suggested by the molecular modelling were verified by the synthesis of the designed molecules and by the evaluation of their in vitro activities against two lung tumour cell lines, A549 and H226. 2-{(E)-2-[5'-(Dibutylamino)-2,2'-bithien-5-yl]vinyl}-1-methylquinolinium iodide exhibited in vitro antiproliferative activity two orders of magnitude higher than that of the most active compound previously synthesized in our laboratory.
Copyright © 2011 Elsevier Masson SAS. All rights reserved.

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Year:  2011        PMID： 22119128     DOI： 10.1016/j.ejmech.2011.10.060

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


  5 in total

1.  A QSPR approach to the ecotoxicity of ionic liquids (Vibrio fischeri) using VolSurf principal properties.

Authors:  Alessio Paterno'; Salvatore Scire; Giuseppe Musumarra
Journal:  Toxicol Res (Camb)       Date:  2016-04-21       Impact factor: 3.524

2.  In vitro combined treatment with cetuximab and trastuzumab inhibits growth of colon cancer cells.

Authors:  T Luca; V Barresi; G Privitera; N Musso; M Caruso; D F Condorelli; S Castorina
Journal:  Cell Prolif       Date:  2014-08-08       Impact factor: 6.831

3.  Amphiphilicity-Controlled Localization of Red Emitting Bicationic Fluorophores in Tumor Cells Acting as Bio-Probes and Anticancer Drugs.

Authors:  Alessio Cesaretti; Letizia Mencaroni; Carmela Bonaccorso; Valentina Botti; Eleonora Calzoni; Benedetta Carlotti; Cosimo Gianluca Fortuna; Nicolò Montegiove; Anna Spalletti; Fausto Elisei
Journal:  Molecules       Date:  2022-06-09       Impact factor: 4.927

4.  Heteroaryl-Ethylenes as New Effective Agents for High Priority Gram-Positive and Gram-Negative Bacterial Clinical Isolates.

Authors:  Dalida Angela Bivona; Alessia Mirabile; Carmelo Bonomo; Paolo Giuseppe Bonacci; Stefano Stracquadanio; Andrea Marino; Floriana Campanile; Carmela Bonaccorso; Cosimo Gianluca Fortuna; Stefania Stefani; Nicolò Musso; Dafne Bongiorno
Journal:  Antibiotics (Basel)       Date:  2022-06-03

5.  Reversible photoswitching of the DNA-binding properties of styrylquinolizinium derivatives through photochromic [2 + 2] cycloaddition and cycloreversion.

Authors:  Sarah Kölsch; Heiko Ihmels; Jochen Mattay; Norbert Sewald; Brian O Patrick
Journal:  Beilstein J Org Chem       Date:  2020-01-23       Impact factor: 2.883
  5 in total

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