77544-60-6Relevant academic research and scientific papers
Lysine-Based C60-Fullerene Nanoconjugates for Monomethyl Fumarate Delivery: A Novel Nanomedicine for Brain Cancer Cells
Kumar, Manish,Sharma, Gajanand,Kumar, Rajendra,Singh, Bhupinder,Katare, Om Prakash,Raza, Kaisar
, p. 2134 - 2142 (2018)
In the present study, water-soluble lysine-based C60-fullerene nanoconjugates (CF-LYS-TEG-MMF) were synthesized using a biodegradable linker for the better delivery of monomethyl fumarate (MMF) employing Prato reaction. CF-LYS-TEG-MMF resulted
1H NMR investigation of solvent effects in aromatic stacking interactions
Cubberley,Iverson
, p. 7560 - 7563 (2001)
One of the marquis challenges in modern Organic Chemistry concerns the design and synthesis of abiotic compounds that emulate the exquisite complex structures and/or functions of biological macromolecules. Oligomers possessing the propensity to adopt well-defined compact conformations, or foldamers, have been attained utilizing hydrogen bonding, torsional restriction, and solvophobic interactions. In this laboratory, aromatic electron donor-acceptor interactions have been exploited in the design of aedamers-foldamers that adopt a novel, pleated secondary structure in aqueous solution. Herein is reported detailed 1H NMR binding studies of aedamer monomers that were carried out in solvents and solvent mixtures covering a broad polarity range. Curve-fitting analysis of the binding data using a model that incorporated the formation of higher order and self-associated complexes yielded a linear free energy relationship between the free energy of complexation and the empirical solvent polarity parameter, ET(30). From these studies, the association of electron-rich and electron-deficient aedamer monomers was seen to be driven primarily by hydrophobic interactions in polar solvents. However, the magnitude of these interactions is modulated to a significant extent by the geometry of the donor-acceptor complex, which, in turn, is dictated by the electrostatic complementarity between the electron-deficient and electron-rich aromatic faces of the monomers.
Honeycomb membranes prepared from 3-O-amino acid functionalized cellulose derivatives
Xu, William Z.,Bar-Nir, Batia Ben-Aroya,Kadla, John F.
, p. 126 - 134 (2014)
The development of value-added wood-derived polymer products is of significant importance. Of particular interest is the synthesis of advanced bioactive cellulosic materials. In the present research, novel cellulosic honeycomb films are reported. Cellulos
A novel biocompatible europium ligand for sensitive time-gated immunodetection
Sayyadi, Nima,Connally, Russell E.,Try, Andrew
, p. 1154 - 1157 (2016)
We describe the synthesis of a novel hydrophilic derivative of a tetradentate β-diketone europium ligand that was used to prepare an immunoconjugate probe against Giardia lamblia cysts. We used a Gated Autosynchronous Luminescence Detector (GALD) to obtain high quality delayed luminescence images of cells 30-fold faster than ever previously reported.
Vesicle aggregation by multivalent ligands: Relating crosslinking ability to surface affinity
Wang, Xi,Mart, Robert J.,Webb, Simon J.
, p. 2498 - 2505 (2007)
In an effort to improve the stability of our tissue-mimetic vesicle aggregates, we have investigated how increasing the valency of our multivalent crosslinking ligand, poly-l-histidine, affected both the extent of vesicle aggregation and the affinity of t
Catalytic Asymmetric Direct-Type 1,4-Addition Reactions of Simple Amides
Suzuki, Hirotsugu,Sato, Io,Yamashita, Yasuhiro,Kobayashi, Shu
, p. 4336 - 4339 (2015)
The development of catalytic asymmetric direct-type reactions of less acidic carbonyl compounds such as amides and esters has been a challenging theme in organic chemistry for decades. Here we describe the asymmetric direct 1,4-addition reactions of simple amides with α,β-unsaturated carbonyl compounds using a catalytic amount of a novel chiral catalyst consisting of a potassium base and a macrocyclic chiral crown ether. The desired 1,5-dicarbonyl compounds were obtained in high yields with excellent diastereo- and enantioselectivities. This is the first example of a highly enantioselective catalytic direct-type reaction of simple amides. In addition, the structure of the chiral potassium catalyst has been investigated by X-ray crystallographic, dynamic 1H NMR, and MALDI-TOF MS analyses.
BisPNA targeting to DNA: Effect of neutral loop on DNA duplex strand invasion by aepPNA-N7G/aepPNA-C substituted peptide nucleic acids
Shirude, Pravin S.,Kumar, Vaijayanti A.,Ganesh, Krishna N.
, p. 5207 - 5215 (2005)
N7-Alkyl-substituted guanine (N7G) as a CH+ mimic has been introduced into aminoethylglycyl PNA (aegPNA) forming a hairpin through a neutral linker derived from bis(tetraethylene) glycol (teg-teg). These form pH-independent PNA2:DNA
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)
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.
Precise macroscopic supramolecular assembly of photopatterned hydrogels
Bao, Chunyan,Pang, Shihao,Wang, Xuebin,Xiang, Yanxing,Xue, Yuan,Ye, Kai,Zhu, Linyong
, p. 8786 - 8789 (2021)
Here we demonstrate that a precise macroscopic supramolecular assembly (MSA) can be achieved using a surface photopatterning strategy. The electrostatic interaction of the photopatterned polyelectrolytes drives hydrogel cuboids to form a stable MSA on a m
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.
