Efficient DNA Click Reaction Replaces Enzymatic Ligation

2019 ◽  
Vol 31 (3) ◽  
pp. 507-512
Author(s):  
Michael Kollaschinski ◽  
Jessica Sobotta ◽  
Alexander Schalk ◽  
Thomas Frischmuth ◽  
Birgit Graf ◽  
...  
Keyword(s):  
Click Reaction ◽  
Enzymatic Ligation

Synthetic Routes for 1,4-disubstituted 1,2,3-triazoles: A Review

2019 ◽  
Vol 23 (8) ◽  
pp. 860-900 ◽  
Author(s):  
Chander P. Kaushik ◽  
Jyoti Sangwan ◽  
Raj Luxmi ◽  
Krishan Kumar ◽  
Ashima Pahwa
Keyword(s):  
Solid Phase ◽  
Click Reaction ◽  
Biological Activities ◽  
Triazole Ring ◽  
Copper Catalysts ◽  
Biologically Active ◽  
Pharmaceutical Chemistry ◽  
Biological Targets ◽  
Synthetic Routes ◽  
High Yields

N-Heterocyclic compounds like 1,2,3-triazoles serve as a key scaffolds among organic compounds having diverse applications in the field of drug discovery, bioconjugation, material science, liquid crystals, pharmaceutical chemistry and solid phase organic synthesis. Various drugs containing 1,2,3-triazole ring which are commonly available in market includes Rufinamide, Cefatrizine, Tazobactam etc., Stability to acidic/basic hydrolysis along with significant dipole moment support triazole moiety for appreciable participation in hydrogen bonding and dipole-dipole interactions with biological targets. Huisgen 1,3-dipolar azide-alkyne cycloaddition culminate into a mixture of 1,4 and 1,5- disubstituted 1,2,3-triazoles. In 2001, Sharpless and Meldal came across with a copper(I) catalyzed regioselective synthesis of 1,4-disubstituted 1,2,3-triazoles by cycloaddition between azides and terminal alkynes. This azide-alkyne cycloaddition has been labelled as a one of the important key click reaction. Click synthesis describes chemical reactions that are simple to perform, gives high selectivity, wide in scope, fast reaction rate and high yields. Click reactions are not single specific reaction, but serve as a pathway for construction of simple to complex molecules from a variety of starting materials. In the last few decades, 1,2,3-triazoles attracted attention of researchers all over the world because of their broad spectrum of biological activities. Keeping in view the biological importance of 1,2,3-triazole, in this review we focus on the various synthetic routes for the syntheisis of 1,4-disubstituted 1,2,3-triazoles. This review involves various synthetic protocols which involves copper and non-copper catalysts, different solvents as well as substrates. It will boost synthetic chemists to explore new pathway for the development of newer biologically active 1,2,3-triazoles.

Green and Facile Synthesis of 1,4-Disubstituted 1,2,3-Triazoles via a Click Reaction of α-Bromo Ketones, [bmim]N3 and Terminal Acetylenes

2013 ◽  
Vol 10 (10) ◽  
pp. 738-743 ◽  
Author(s):  
Azadeh Fazeli ◽  
Hossein Oskooie ◽  
Yahya Beheshtiha ◽  
Majid Heravi ◽  
Hassan Valizadeh
Keyword(s):  
Click Reaction ◽  
Facile Synthesis ◽  
Terminal Acetylenes

Tuning DNA Stability To Achieve Turnover in Template for an Enzymatic Ligation Reaction

2011 ◽  
Vol 50 (38) ◽  
pp. 8922-8926 ◽  
Author(s):  
Abu Kausar ◽  
Rosalie D. McKay ◽  
Jade Lam ◽  
Rohan S. Bhogal ◽  
Alexandra Y. Tang ◽  
...  
Keyword(s):  
Dna Stability ◽  
Ligation Reaction ◽  
Enzymatic Ligation

scholarly journals Photo Click Reaction of Acylsilanes with Indoles

2021 ◽  
Author(s):  
Constantin Stuckhardt ◽  
Maren Wissing ◽  
Armido Studer
Keyword(s):  
Click Reaction

scholarly journals Enhancing Toughness and Reducing Volumetric Shrinkage for Bis-GMA/TEGDMA Resin Systems by Using Hyperbranched Thiol Oligomer HMDI-6SH

Materials ◽  
2021 ◽  
Vol 14 (11) ◽  
pp. 2817
Author(s):  
Biao Yu ◽  
Jingwei He ◽  
Sufyan Garoushi ◽  
Pekka K. Vallittu ◽  
Lippo Lassila
Keyword(s):  
Water Sorption ◽  
Water Solubility ◽  
Click Reaction ◽  
Raw Materials ◽  
Triethylene Glycol ◽  
Bending Test ◽  
Volumetric Shrinkage ◽  
Dental Resin ◽  
System A ◽  
Double Bond Conversion

In order to improve the toughness and reduce polymerization shrinkage of traditional bisphenol A-glycidyl methacrylate (Bis-GMA)/triethylene glycol dimethacrylate (TEGDMA) based dental resin system, a hyperbranched thiol oligomer (HMDI-6SH) was synthesized via thiol-isocyanate click reaction using pentaerythritol tetra(3-mercaptopropionate (PETA) and dicyclohexylmethane 4,4′-diisocyanate (HMDI) as raw materials. Then HMDI-6SH was mixed with 1,3,5-Triallyl-1,3,5-Triazine-2,4,6(1H,3H,5H)-Trione (TTT) to prepare thiol-ene monomer systems, which were added into Bis-GMA/TEGDMA resins with different mass ratio from 10 wt% to 40 wt% to serve as anti-shrinking and toughening agent. The physicochemical properties of these thiol-ene-methacrylate ternary resins including functional groups conversion, volumetric shrinkage, flexural properties, water sorption, and water solubility were evaluated. The results showed that the incorporation of HMDI/TTT monomer systems into Bis-GMA/TEGDMA based resin could improve C=C double bond conversion from 62.1% to 82.8% and reduced volumetric shrinkage from 8.53% to 4.92%. When the mass fraction of HMDI/TTT monomer systems in the resins was no more than 20 wt%, the flexural strength of the resin was higher or comparable to Bis-GMA/TEGDMA based resins (p > 0.05). The toughness (it was measured from the stress–strain curves of three-point bending test) of the resins was improved. Water sorption and water solubility tests showed that the hydrophobicity of resin was enhanced with increasing the content of thioester moiety in resin.

scholarly journals Controllable Drug Delivery by Na+/K+ ATPase α1 Targeting Peptide Conjugated DSPE-PEG Nanocarriers for Breast Cancer

2021 ◽  
Vol 20 ◽  
pp. 153303382110278
Author(s):  
Yayan Yang ◽  
Qian Feng ◽  
Chuanfeng Ding ◽  
Wei Kang ◽  
Xiufeng Xiao ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Drug Delivery ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Click Reaction ◽  
Chemotherapy Drugs ◽  
Targeting Peptide ◽  
And Migration

Although Epirubicin (EPI) is a commonly used anthracycline for the treatment of breast cancer in clinic, the serious side effects limit its long-term administration including myelosuppression and cardiomyopathy. Nanomedicines have been widely utilized as drug delivery vehicles to achieve precise targeting of breast cancer cells. Herein, we prepared a DSPE-PEG nanocarrier conjugated a peptide, which targeted the breast cancer overexpression protein Na+/K+ ATPase α1 (NKA-α1). The nanocarrier encapsulated the EPI and grafted with the NKA-α1 targeting peptide through the click reaction between maleimide and thiol groups. The EPI was slowly released from the nanocarrier after entering the breast cancer cells with the guidance of the targeting NKA-α1 peptide. The precise and controllable delivery and release of the EPI into the breast cancer cells dramatically inhibited the cells proliferation and migration in vitro and suppressed the tumor volume in vivo. These results demonstrate significant prospects for this nanocarrier as a promising platform for numerous chemotherapy drugs.

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