Universität zu Köln

Thomopoulou, Persefoni, Sachs, Julia, Teusch, Nicole ORCID: 0000-0002-9030-1493, Mariappan, Aruljothi, Gopalakrishnan, Jay and Schmalz, Hans-Guenther ORCID: 0000-0003-0489-1827 (2016). New Colchicine-Derived Triazoles and Their Influence on Cytotoxicity and Microtubule Morphology. ACS Med. Chem. Lett., 7 (2). S. 188 - 192. WASHINGTON: AMER CHEMICAL SOC. ISSN 1948-5875

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Abstract

A series of new colchicinoids with a variable triazole unit at C-7 was synthesized through Cu(I)-catalyzed 1,3-dipolar cycloaddition (click-chemistry) of a colchicine-derived azide with various alkynes and the cytotoxicity against THP-1 and Jurkat cancer cell lines was used for structural optimization. Three particularly active compounds (IC50 <= 5 nM) were additionally investigated with respect to their efficacy against relevant solid tumor cell lines (HeLa, A549, and SK MES 1). Besides distorting the microtubule morphology by tubulin depolymerization, one compound also exhibited a pronounced centrosome declustering effect in triple negative breast cancer cells (MDA-MB-231) and nonsmall cell lung cancer cells (H1975).

Item Type:	Journal Article
Creators:	Creators Email ORCID ORCID Put Code Thomopoulou, Persefoni UNSPECIFIED UNSPECIFIED UNSPECIFIED Sachs, Julia UNSPECIFIED UNSPECIFIED UNSPECIFIED Teusch, Nicole UNSPECIFIED orcid.org/0000-0002-9030-1493 UNSPECIFIED Mariappan, Aruljothi UNSPECIFIED UNSPECIFIED UNSPECIFIED Gopalakrishnan, Jay UNSPECIFIED UNSPECIFIED UNSPECIFIED Schmalz, Hans-Guenther UNSPECIFIED orcid.org/0000-0003-0489-1827 UNSPECIFIED
URN:	urn:nbn:de:hbz:38-286024
DOI:	10.1021/acsmedchemlett.5b00418
Journal or Publication Title:	ACS Med. Chem. Lett.
Volume:	7
Number:	2
Page Range:	S. 188 - 192
Date:	2016
Publisher:	AMER CHEMICAL SOC
Place of Publication:	WASHINGTON
ISSN:	1948-5875
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 BIOLOGICAL EVALUATION; TUBULIN; AGENTS; BIOLUMINESCENCE; ANALOGS; AZIDES; ENTRY; ATP Multiple languages Chemistry, Medicinal Multiple languages
Refereed:	Yes
URI:	http://kups.ub.uni-koeln.de/id/eprint/28602