77544-68-4Relevant articles and documents
Phthalimide–Oxy Derivatives for 3′- or 5′-Conjugation of Oligonucleotides by Oxime Ligation and Circularization of DNA by “Bis- or Tris-Click” Oxime Ligation
Meyer, Albert,Vasseur, Jean-Jacques,Dumy, Pascal,Morvan, Fran?ois
, p. 6931 - 6941 (2017)
A solid support and two phosphoramidites exhibiting a phthalimide–oxy group were synthesized. First, after treatment with hydrazine, the resulting 5′- and 3′-oxyamine oligonucleotides were conjugated with aldehyde derivatives by oxime ligation. Second, ol
In Vitro Photodynamic Studies of a BODIPY-Based Photosensitizer
Kim, Bosung,Sui, Binglin,Yue, Xiling,Tang, Simon,Tichy, Michael G.,Belfield, Kevin D.
, p. 25 - 28 (2017)
A new halogenated 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene (BODIPY) derivative was designed as a singlet-oxygen photosensitizer (PS) for use as a photodynamic therapy (PDT) agent, and its photophysical properties were characterized. The PS, having two i
The dynamic covalent reaction based on diselenide-containing crown ether irradiated by visible light
Shang, Jie,Gong, Hanlin,Zhang, Qian,Cui, Zhiliyu,Li, Shuangran,Lv, Ping,Pan, Tiezheng,Ge, Yan,Qi, Zhenhui
, p. 2005 - 2008 (2021)
A novel diselenide-containing crown ether (BC7Se2) was fabricated, which can polymerize to form cyclic oligomers through intermolecular dynamic covalent reaction by irradiation of visible light. The size and distribution of oligomers are relate
Discovery of novel potent covalent inhibitor-based EGFR degrader with excellent in vivo efficacy
Cui, Jiaqi,Du, Yu,Huang, Lei,Niu, Jing,Shi, Shi,Xu, Yungen,Zhu, Qihua
supporting information, (2022/01/26)
Although several Epidermal growth factor receptor (EGFR) inhibitors have been approved for the treatment of non-small-cell lung cancers (NSCLC), acquired drug resistance and side effects largely encumbered their application in clinic. The emerging technology Proteolysis targeting chimera (PROTAC) could be an alternative strategy to overcome these problems. Here, we reported the discovery of Dacomitinib-based EGFR degraders. Promising compound 13 can effectively induce degradation of EGFRdel19 with DC50 value of 3.57 nM in HCC-827 cells, but not to other EGFR mutant, wild-type EGFR protein and the same family receptors (HER2 and HER4). Of note, 13 is the first EGFR-PROTAC to evaluate antitumor effect in vivo, and exhibited excellent antitumor efficacy (TGI = 90%) at a dose of 30 mg/kg without causing observable toxic effects. The preliminary mechanism study demonstrated that 13 can efficiently induce EGFR protein degradation through ubiquitin proteasome pathway and inhibit phosphorylation of downstream pathways in vitro and in vivo, which indicated that 13 exerted antitumor effect by degradation of EGFR protein in tumor tissue. Overall, our study provided further evidence to validate EGFR-PROTACs as a promising strategy for lung cancer therapy.
Selenacrown Macrocycle in Aqueous Medium: Synthesis, Redox-Responsive Self-Assembly, and Enhanced Disulfide Formation Reaction
Shang, Jie,Li, Bo,Shen, Xin,Pan, Tiezheng,Cui, Zhiliyu,Wang, Yangxin,Ge, Yan,Qi, Zhenhui
, p. 1430 - 1436 (2021/01/13)
Organic selenides are famous for their coordination and catalytic functions in the organic phase, albeit challenging for aqueous medium. Herein, the combination of a hydrophilic body of crown ether and substitution of one oxygen atom with a selenium one provides a new type of design route for organic selenide entities with charming functions in aqueous solution. The selenacrown ether C9Se presented here intrinsically shows an amphiphile-like property. Its nanosphere structure in water readily expands the catalysis of organic selenide to aqueous substrates in thiol/disulfide conversion.
