34264-14-7Relevant articles and documents
Synthesis and X-ray structural investigation of 1,3,5-trisbenzene
Lindeman, S. V.,Dvorikova, R. A.,Gol'din, I. R.,Struchkov, Yu. T.,Teplyakov, M. M.
, p. 1536 - 1539 (1993)
Synthesis and X-ray structural investigation of 1,3,5-trisbenzene (1) were carried out.Compound 1 is a trifunctional monomer for the synthesis of crosslinked polymers and a model of a section of polymeric network of this kind.In a
Bis-Organosilicon based receptor for detection of Hg2+ ions: Low detection limit and excellent selectivity
Chowdhary, Kavita,Mohit,Satija, Pinky,Sharma, Geetika,Shilpy,Singh, Akshpreet,Singh, Gurjaspreet,Singh, Jandeep,Singh, Jasbhinder
, (2020)
Mercury Contamination represents a major environmental and health concern for which new eco-friendly solutions are desired. Azide–alkyne cycloaddition and Claisen Schmidt reaction were attempted to trigger a flavanone based bis-siloxyl hybrid materials. T
Peroxide- And transition metal-free electrochemical synthesis of α,β-epoxy ketones
Zhang, Mengxun,Chen, Tie,Fang, Shisong,Wu, Weihua,Wang, Xin,Wu, Haiqiang,Xiong, Yongai,Song, Jun,Li, Chenyang,He, Zhendan,Lee, Chi-Sing
supporting information, p. 2481 - 2486 (2021/04/02)
A novel electrochemical method for the synthesis of α,β-epoxy ketones is reported. With KI as the redox mediator, methyl ketones reacted with aldehydes under peroxide- and transition metal-free electrolytic conditions and afforded α,β-epoxy ketones in one pot (36 examples, 52-90% yield). This safe and environmental-friendly method has a broad substrate scope and can readily provide a variety of α,β-epoxy ketones in gram-scales for evaluation of their anti-cancer activities.
Strategic Design of Catalytic Lysine-Targeting Reversible Covalent BCR-ABL Inhibitors**
Anantharajan, Jothi,Baburajendran, Nithya,Foo, Klement,Joy, Joma K.,Keller, Thomas H.,Kwek, Perlyn Z.,Li, Rong,Liu, Boping,Poulsen, Anders,Quach, David,Retna, Priya,Tang, Guanghui,Tee, Doris H. Y.,Wee, John L. K.,Yang, Wan-Qi,Yao, Shao Q.,Zhang, Chong-Jing
supporting information, p. 17131 - 17137 (2021/06/28)
Targeted covalent inhibitors have re-emerged as validated drugs to overcome acquired resistance in cancer treatment. Herein, by using a carbonyl boronic acid (CBA) warhead, we report the structure-based design of BCR-ABL inhibitors via reversible covalent targeting of the catalytic lysine with improved potency against both wild-type and mutant ABL kinases, especially ABLT315I bearing the gatekeeper residue mutation. We show the evolutionarily conserved lysine can be targeted selectively, and the selectivity depends largely on molecular recognition of the non-covalent pharmacophore in this class of inhibitors, probably due to the moderate reactivity of the warhead. We report the first co-crystal structures of covalent inhibitor-ABL kinase domain complexes, providing insights into the interaction of this warhead with the catalytic lysine. We also employed label-free mass spectrometry to evaluate off-targets of our compounds at proteome-wide level in different mammalian cells.