84322-60-1Relevant academic research and scientific papers
Chemical trigger-enabled bioconjugation reaction
Cao, Yu,Du, Juanjuan,Jia, Xiangqian,Jiang, Haolin,Tang, Yefeng,Wu, Yunfei,Xie, Fayang,Yang, Hongzhi,Zhou, Bing,Zhu, Rui,Zhu, Zhu
supporting information, p. 8343 - 8351 (2021/10/12)
Development of conceptually novel and practically useful bioconjugation reactions has been an intense pursuit of chemical biology research. Herein, we report an unprecedented bioconjugation reaction that hinges on a chemical trigger-enabled inverse-electron-demand Diels-Alder (IEDDA) cycloaddition oftrans-cycloheptene (TCH) with tetrazine. Unlike the conventional strain-promoted bioconjugation reactions that utilize built-in strained alkenes as reactants, the current one features a “trigger-release-conjugate” reaction model, in which a highly strained TCH species is released from a bench-stable bicyclicN-nitrosourea (BNU) derivative upon treatment with an external stimulus. It is noteworthy that the reactivity-stability balance of BNU derivatives could be tuned by manipulating their N-1 substituents. As a proof-of-concept case, this new chemical trigger-enabled IEDDA reaction has been applied toin vitroprotein labeling and pretargeted cell imaging. This work opens a new avenue to utilize BNU derivatives as a new class of chemical reporters in bioconjugate chemistry.
Bicyclo[4.1.0]heptane nitrosourea derivative for biological orthogonal reaction, and preparation method and application thereof
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Paragraph 0071-0072, (2020/06/02)
The invention discloses a bicyclo[4.1.0]heptane nitrosourea derivative for a biological orthogonal reaction, and a preparation method and an application thereof. The structural formula of the bicyclo[4.1.0]heptane nitrosourea derivative is represented by
Novel indolobenzazepine derivatives, useful as tranquilizers
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, (2008/06/13)
Certain novel 1,2,3,4,8,9-hexahydro-3-(substituted)pyrido[4',3':2,3]indolo[1,7-ab][1]-benzazepines are useful as minor tranquilizers (anxiolytics) and/or major tranquilizers (antipsychotics). The minor tranquilizers are effective at non-ataxic doses, and are not likely to cause addiction when abused. A representative compound in this class is 3-(cyclopropylmethyl)-1,2,3,4,8,9-hexahydropyrido[4',3':2,3]indolo[1,7-ab][1]benzazepine.
