118887-70-0Relevant articles and documents
Synthesis and biological evaluation of a new class of triazin-triazoles as potential inhibitors of human farnesyltransferase
Lucescu, Liliana,Bcu, Elena,Belei, Dalila,Shova, Sergiu,Rigo, Benot,Gautret, Philippe,Dubois, Jolle,Ghinet, Alina
, p. 1999 - 2021 (2016)
A new synthesis of ethynyldimethoxytriazine 1, an important platform-compound for developing new chemical entities for anticancer research and for other biological applications, is described. Compound 1 was further reacted with azides 5a-i to provide triazin-triazoles 2a-i, which were tested on human farnesyltransferase and on the NCI-60 human tumor cell lines. Synthesis of other dimethoxytriazine derivatives 15 and 16, linked to a sp 2 or a sp 3 carbon atom were also studied. Graphical Abstract: [Figure not available: see fulltext.]
A novel and efficient method for the synthesis of α-azidoketones and α-ketothiocyanates
Yadav,Subba Reddy,Srinivas
, p. 882 - 883 (2004)
α-Diazoketones underwent insertion smoothly with sodium azide and potassium thiocyanate in the presence of CeCl3 ·7H 2O under mild reaction conditions to afford the corresponding α-azidoketones and α-ketothiocyanates in excellent yields.
Polymer-supported hypervalent iodine reagent mediated synthesis of α-azidoketones
Wang, Huey-Min,Hou, Rei-Sheu,Wu, Jian-Long,Chen, Ling-Ching
, p. 1333 - 1335 (2007)
The reaction of aryl ketones with sodium azide using polymer-supported bis(trifluoroacetoxyiodo)-benzene (PSBTI) in the presence of trifluoroacetic acid (TFA) to prepare α-azidoketones in one-pot conditions is reported.
A fast procedure for the preparation of vicinal azidoalcohols using polymer supported reagents
Souza Brenelli, Eugênia Cristina,Brenelli, José Afranio,Laranjeira Pinto, Raquel Cristina
, p. 4531 - 4533 (2005)
Several vicinal azidoalcohols were prepared in good to high yield and purity, starting from aryl α-haloketones, using reagents supported on a macroporous ion exchange resin. This is a fast and new approach to aryl azidoalcohols.
Visible-light-enabled oxyazidation of alkenes leading to α-azidoketones in air
Wei, Wei,Cui, Huanhuan,Yue, Huilan,Yang, Daoshan
, p. 3197 - 3202 (2018)
A new and facile visible-light-enabled method for the synthesis of α-azidoketones has been developed via oxyazidation of alkenes with TMSN3 in air at room temperature. A series of α-azidoketones could be easily and efficiently obtained in moder
Electrochemical Difunctionalization of Styrenes via Chemoselective Oxo-Azidation or Oxo-Hydroxyphthalimidation
Jiang, Haobin,Wang, Feng,Ye, Zenghui,Zhang, Fengzhi,Zhu, Rongjin
supporting information, p. 8240 - 8245 (2021/11/17)
Atom- and step-economic oxo-azidation and oxo-hydroxyphthalimidation of styrenes have been developed under mild electrolytic conditions, respectively. Various valuable alpha-azido or hydroxyphthalimide aromatic ketones were synthesized efficiently from readily available styrenes, azides, and N-hydroxyphthalimides. Mechanism studies show that two different pathways involved in these two transformations.
Novel series of triazole containing coumarin and isatin based hybrid molecules as acetylcholinesterase inhibitors
Bedi, Preet Mohinder Singh,Bhagat, Kavita,Gulati, Harmandeep Kaur,Kaur, Arshmeet,Kumar, Nitish,Sharma, Aakriti,Singh, Atamjit,Singh, Harbinder,Singh, Jatinder Vir
, (2021/07/28)
Novel series of coumarin-triazole and isatin-triazole hybrids were rationally designed, synthesized and biologically evaluated to check their inhibitory potential against acetylcholinesterase enzyme by using in vitro Ellman's method. Most of the hybrid compounds showed significant inhibition against the enzyme. Biological assay revealed that compound B-1 (among 4-hydroxycoumarin-triazole series) and compound AS-8 (from isatin-triazole series) possessed potent inhibitory activity against the AChE with the IC50 values of 110 ± 1.11 nM and 155 ± 1.65 nM, respectively. These active compounds (B-1 and AS-8) exhibited mixed mode of enzyme's inhibition which was confirmed through enzyme kinetic studies. Molecular docking studies were performed to understand the binding modes of these potent compounds within the active pocket of AChE enzyme by using Discovery studio. Furthermore, to predict the stability of the most prominent compound B-1 within the catalytic cavity of AChE, molecular dynamic simulations were performed for 5 ns and was found that ligand and protein complex is stable within their dynamic system. Therefore, these hybrids could be taken as effective lead candidates for further designing, development and optimization of new acetylcholinesterase inhibitors.
