Universität zu Köln

Gracheva, Iuliia A., Voitovich, Iuliia V., Faerman, Vladimir I., Sitnikov, Nikolay S., Myrsikova, Ekaterina V., Schmalz, Hans-Gunther ORCID: 0000-0003-0489-1827, Svirshevskaya, Elena V. and Fedorov, Alexey Yu (2017). Synthesis and cytostatic properties of polyfunctionalized furanoallocolchicinoids. Eur. J. Med. Chem., 126. S. 432 - 444. PARIS: ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER. ISSN 1768-3254

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Abstract

A series of furan-based allocolchicinoids was prepared from commercially available colchicine via a nine step reaction sequence. Cytostatic activity, cell cycle arrest, apoptosis, tubulin and F-actin expression were studied in vitro in 2D and 3D cultures of normal and tumor epithelial keratinocytes, endothelial and mesenchymal cells. Among the prepared furanoallocolchicine analogues, 14a and 7a displayed the most pronounced anti-cancer activity. These compounds induced two types of effects: (a) cell cycle arrest in the G2/M phase as a direct consequence of effective tubulin binding (metaphase effect), and (b) pronounced cell stress (as evidenced by the overexpression of tubulin and F-actin), which was caused by the hyperpolarization of mitochondrial and lysosomal membranes (interphase effect). 2016 Elsevier Masson SAS. All rights reserved.

Item Type:	Journal Article
Creators:	Creators Email ORCID ORCID Put Code Gracheva, Iuliia A. UNSPECIFIED UNSPECIFIED UNSPECIFIED Voitovich, Iuliia V. UNSPECIFIED UNSPECIFIED UNSPECIFIED Faerman, Vladimir I. UNSPECIFIED UNSPECIFIED UNSPECIFIED Sitnikov, Nikolay S. UNSPECIFIED UNSPECIFIED UNSPECIFIED Myrsikova, Ekaterina V. UNSPECIFIED UNSPECIFIED UNSPECIFIED Schmalz, Hans-Gunther UNSPECIFIED orcid.org/0000-0003-0489-1827 UNSPECIFIED Svirshevskaya, Elena V. UNSPECIFIED UNSPECIFIED UNSPECIFIED Fedorov, Alexey Yu UNSPECIFIED UNSPECIFIED UNSPECIFIED
URN:	urn:nbn:de:hbz:38-242159
DOI:	10.1016/j.ejmech.2016.11.020
Journal or Publication Title:	Eur. J. Med. Chem.
Volume:	126
Page Range:	S. 432 - 444
Date:	2017
Publisher:	ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
Place of Publication:	PARIS
ISSN:	1768-3254
Language:	English
Faculty:	Faculty of Mathematics and Natural Sciences
Divisions:	Faculty of Mathematics and Natural Sciences > Department of Chemistry > Institute of Organic Chemistry
Subjects:	no entry
Uncontrolled Keywords:	Keywords Language FAMILIAL MEDITERRANEAN FEVER; COMBRETASTATIN A-4 ANALOGS; PRIMARY BILIARY-CIRRHOSIS; COLCHICINE BINDING-SITE; ANTICANCER AGENTS; BIOLOGICAL EVALUATION; RECURRENT PERICARDITIS; 4-ARYLCOUMARIN ANALOGS; ANTINEOPLASTIC AGENTS; TUBULIN Multiple languages Chemistry, Medicinal Multiple languages
Refereed:	Yes
URI:	http://kups.ub.uni-koeln.de/id/eprint/24215