Cancer is a class of formidable disease with high degree of mortality. Despite much progress in chemotherapy, the problem of drug resistance has led to the search for newer leads with superior efficacy. 1,2,3- Triazoles are among a vast number of nitrogen containing heterocycles studied extensively as pharmacologically important scaffolds. Recently developed copper(I)-catalyzed cycloaddition reaction between organic azides and terminal alkynes yielding 1,4-disubstituted 1,2,3-triazoles has attracted considerable attention because it allows the construction of a vast array of 1,2,3-triazoles with significant potential in pharmaceutical chemistry. In this article, an attempt to summarize the wide range of anticancer agents derived from copper(I)-catalyzed azide alkyne cycloaddition reported by the authors worldwide, has been made. This review includes articles published from 2010 onwards and summarizes the recent progress on the development of 1,4-disubstituted 1H-1,2,3-triazoles as novel anticancer chemotypes with high therapeutic indices.
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http://dx.doi.org/10.2174/1871520616666160811113531 | DOI Listing |
Chin J Nat Med
December 2023
School of Pharmacy, Hangzhou Normal University, Hangzhou 311121, China; Key Laboratory of Elemene Class Anti-cancer Chinese Medicines; Engineering Laboratory of Development and Application of Traditional Chinese Medicines; Collaborative Innovation Center of Traditional Chinese Medicines of Zhejiang Province, Hangzhou Normal University, Hangzhou 311121, China. Electronic address:
Natural products are essential sources of antitumor drugs. One such molecule, β-elemene, is a potent antitumor compound extracted from Curcuma wenyujin. In the present investigation, a series of novel 13,14-disubstituted nitric oxide (NO)-donor β-elemene derivatives were designed, with β-elemene as the foundational compound, and subsequently synthesized to evaluate their therapeutic potential against leukemia.
View Article and Find Full Text PDFOrg Lett
August 2014
Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore, 117543, Singapore.
Two 7,14-disubstituted-5,12-dithiapentacenes (1 and 2) with quinoidal conjugation were synthesized. Their ground-state quinoidal structures were proven by X-ray crystallographic analysis. They showed very different electronic and optical properties from those of the corresponding pentacene derivatives with diene conjugation, and their stability was significantly improved.
View Article and Find Full Text PDFOrg Lett
April 2009
Department of Electronic Chemistry, Interdisciplinary Graduate School of Science and Engineering, Tokyo Institute of Technology, Nagatsuta, Midori-ku, Yokohama 226-8502, Japan.
Title 7,14-disubsituted pentacene-5,12-diones were prepared for the first time by a nucleophilic substitution reaction of a pentacene-5,7,12,14-tetraone with aryl- or ethynyllithiums followed by a dehydroxylation reaction. The methylenequinoid structures with two conjugated carbonyl groups were clearly observed in their crystal structures. They showed intense absorptions in the visible region and amphoteric redox properties with high reduction potentials.
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April 2000
Faculty of Pharmaceutical Sciences, University of Tokushima, Japan.
[figure: see text] A reliable and rigid spacer, trans,trans,trans-perhydronaphthacene, for molecular tweezers was designed. A synthesis and molecular recognition study of its 1,14-disubstituted derivatives was carried out.
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