An efficient one-pot synthesis of heterocycle-fused 1,2,3-triazole derivatives as anti-cancer agents

Bioorganic & Medicinal Chemistry Letters
Sheng-Jiao YanJun Lin

Abstract

A series of heterocycle-fused 1,2,3-triazoles were easily prepared by the 1,3-dipolar cycloaddition of heterocyclic ketene aminals or N,O-acetals with sodium azide and polyhalo isophthalonitriles in a one-pot reaction at room temperature without a catalyst and evaluated in vitro against a panel of human tumour cell lines. 1,3-Oxazoheterocycle fused 1,2,3-triazoles were more potent against the tumour cell lines Skov-3, HL-60, A431, A549 and HepG-2 than 1,3-diazoheterocycle fused 1,2,3-triazoles. 4-Methoxyphenyl substituted 1,3-oxazoheterocycle fused 1,2,3-triazole 6j was found to be the most potent derivative with IC(50) values lower than 1.9 microg/mL against A431 and K562 human tumour cell lines.

References

Dec 17, 2005·Organic & Biomolecular Chemistry·Claire A M Cariou, John S Snaith

❮ Previous
Next ❯

Citations

Mar 27, 2012·Nucleosides, Nucleotides & Nucleic Acids·Iwona E GłowackaAndrzej E Wróblewski
Nov 14, 2013·European Journal of Medicinal Chemistry·Iwona E GłowackaAndrzej E Wróblewski
Jan 28, 2017·Bioorganic Chemistry·Divya DheerRavi Shankar
Apr 23, 2017·Bioorganic & Medicinal Chemistry Letters·Niggula Praveen KumarNagula Shankaraiah
Feb 22, 2013·Archiv der Pharmazie·Iwona E GłowackaAndrzej E Wróblewski
Sep 29, 2011·Chemistry, an Asian Journal·Sandip G AgalaveVandana S Pore
Dec 15, 2011·Organic & Biomolecular Chemistry·Vito FiandaneseGiacomo G Rafaschieri
Mar 14, 2019·Mini Reviews in Medicinal Chemistry·Ankit Jain, Poonam Piplani
Jul 18, 2020·Recent Patents on Anti-cancer Drug Discovery·Katerina I SlavovaIrena P Kostova
Feb 23, 2020·Accounts of Chemical Research·Paramasivam SivaguruXihe Bi

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.