139115-92-7Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of biotin-labeled (-)-ternatin, a potent fat-accumulation inhibitor against 3T3-L1 adipocytes
Shimokawa, Kenichiro,Yamada, Kaoru,Ohno, Osamu,Oba, Yuichi,Uemura, Daisuke
, p. 92 - 95 (2009)
The design, synthesis, and biological activity of biotin-labeled (-)-ternatin are reported. Chemical modification, that is, biotinylation, was conducted using Click chemistry at the 6-position (NMe-d-ProGly moiety), which was a plausible location selected
Design, Synthesis, and Biological Evaluation of Cytochrome P450 1B1 Targeted Molecular Imaging Probes for Colorectal Tumor Detection
Meng, Qingqing,Wang, Zengtao,Cui, Jiahua,Cui, Qing,Dong, Jinyun,Zhang, Qijing,Li, Shaoshun
, p. 10901 - 10909 (2018)
Cytochrome P450 1B1 (CYP1B1) was found to be universally expressed in various tumors. Herein, we reported near-infrared fluorescent imaging probes for tumor detection via visualizing CYP1B1. After introducing the linker to a CYP1B1 selective inhibitor we found previously, we got the resulting compound 5b which kept strong inhibition ability against CYP1B1 (IC50 = 8.7 ± 1.2 nM) and high selectivity. Then, in vitro microscope studies and cell binding assay of probes indicated that the corresponding probe 6b could specifically be accumulated in CYP1B1 overexpressed colorectal cancer cell HCT-15 and showed satisfying binding affinity to target. During the in vivo noninvasive optical imaging, 6b was proved to rapidly lighten tumor in vivo as early as 6 h after injection. This work is the first attempt to visualize CYP1B1 for noninvasive imaging of tumor which could provide new approach for tumor diagnosis.
Nickel Boride Catalyzed Reductions of Nitro Compounds and Azides: Nanocellulose-Supported Catalysts in Tandem Reactions
Proietti, Giampiero,Prathap, Kaniraj Jeya,Ye, Xinchen,Olsson, Richard T.,Dinér, Peter
supporting information, p. 133 - 146 (2021/11/04)
Nickel boride catalyst prepared in situ from NiCl2 and sodium borohydride allowed, in the presence of an aqueous solution of TEMPO-oxidized nanocellulose (0.01 wt%), the reduction of a wide range of nitroarenes and aliphatic nitro compounds. Here we describe how the modified nanocellulose has a stabilizing effect on the catalyst that enables low loading of the nickel salt pre-catalyst. Ni-B prepared in situ from a methanolic solution was also used to develop a greener and facile reduction of organic azides, offering a substantially lowered catalyst loading with respect to reported methods in the literature. Both aromatic and aliphatic azides were reduced, and the protocol is compatible with a one-pot Boc-protection of the obtained amine yielding the corresponding carbamates. Finally, bacterial crystalline nanocellulose was chosen as a support for the Ni-B catalyst to allow an easy recovery step of the catalyst and its recyclability for new reduction cycles.
EXPANSION MICROSCOPY COMPATIBLE ANCHORABLE HandE STAINING FOR HISTOPATHOLOGY
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, (2022/03/18)
The present invention employs the technique for expansion microscopy (E×M) utilizing anchorable derivatives of hematoxylin and eosin (HandE) stained tissue specimens within tissue samples, in order to achieve high resolution detection of biomolecules with precise morphological features of cells and nuclei, which in turn, allows for effective for accurate early stage disease diagnosis including various cancers. Staining with HandE employs anchorable derivatives that can be cross-linked into the E×M hydrogel matrix.
Small molecule compound based on EZH2 protein degradation, and application thereof
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Paragraph 0103-0106, (2021/08/07)
The invention discloses a series of small molecule compounds capable of selectively degrading EZH2 protein, and application thereof. The compounds can be prepared into proper pharmaceutical dosage forms for EZH2-mediated related tumor treatment.
NOVEL AUTOPHAGY-TARGETING CHIMERA (AUTOTAC) COMPOUND, AND COMPOSITION FOR PREVENTING, ALLEVIATING, OR TREATING DISEASES THROUGH TARGET PROTEIN DEGRADATION COMPRISING SAME
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Paragraph 0123; 0128, (2021/06/03)
The present invention relates to a novel AUTOTAC chimeric compound in which a new p62 ligand and a target-binding ligand are connected by a linker, a stereoisomer, hydrate, solvate or prodrug thereof, and a pharmaceutical or food composition for the prevention or treatment of diseases by degrading the target protein including the same as an active ingredient. They can target specific proteins to adjust their concentrations, and can also deliver drugs and other small molecule compounds to lysosomes. The AUTOTAC chimeric compound according to the present invention can be usefully used as a pharmaceutical composition for the prevention, amelioration or treatment of various diseases by selectively eliminating specific proteins.
Heterocyclic compound and application thereof
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Paragraph 1323-1327, (2021/08/07)
The invention discloses a heterocyclic compound and application thereof. The invention provides a heterocyclic compound as shown in a formula I, or pharmaceutically acceptable salt thereof. The heterocyclic compound can be used for degrading ALK, c-Met and ROS proteins.
TARGETED DEGRADERS OF ABERRANT TAU BASED ON THE PET TRACER PBB3
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Paragraph 00144; 00145, (2021/09/26)
Disclosed are bispecific compounds (degraders) that target tau protein for degradation. Also disclosed are pharmaceutical compositions containing the degraders and methods of using the compounds to treat neurodegenerative and neuropsychiatric diseases ass
Self-Assembly and Molecular Recognition in Water: Tubular Stacking and Guest-Templated Discrete Assembly of Water-Soluble, Shape-Persistent Macrocycles
Wang, Qiuhua,Zhong, Yulong,Miller, Daniel P.,Lu, Xiaoxing,Tang, Quan,Lu, Zhong-Lin,Zurek, Eva,Liu, Rui,Gong, Bing
supporting information, p. 2915 - 2924 (2020/02/04)
Supramolecular chemistry in aqueous media is an area with great fundamental and practical significance. To examine the role of multiple noncovalent interactions in controlled assembling and binding behavior in water, the self-association of five water-soluble hexakis(m-phenylene ethynylene) (m-PE) macrocycles, along with the molecular recognition behavior of the resultant assemblies, is investigated with UV-vis, fluorescence, CD, and NMR spectroscopy, mass spectrometry, and computational studies. In contrast to their different extents of self-aggregation in organic solvents, all five macrocycles remain aggregated in water at concentrations down to the micromolar (μM) range. CD spectroscopy reveals that 1-F6 and 1-H6, two macrocycles carrying chiral side chains and capable of H-bonded self-association, assemble into tubular stacks. The tubular stacks serve as supramolecular hosts in water, as exemplified by the interaction of macrocycles 1-H6 and 2-H6 and guests G1 through G4, each having a rod-like oligo(p-phenylene ethynylene) (p-PE) segment flanked by two hydrophilic chains. Fluorescence and 1H NMR spectroscopy revealed the formation of kinetically stable, discrete assemblies upon mixing 2-H6 and a guest. The binding stoichiometry, determined with fluorescence, 1H NMR, and ESI-MS, reveals that the discrete assemblies are novel pseudorotaxanes, each containing a pair of identical guest molecules encased by a tubular stack. The two guest molecules define the number of macrocyclic molecules that comprise the host, which curbs the "infinite" stack growth, resulting in a tubular stack with a cylindrical pore tailoring the length of the p-PE segment of the bound guests. Each complex is stabilized by the action of multiple noncovalent forces including aromatic stacking, side-chain H-bonding, and van der Waals interactions. Thus, the interplay of multiple noncovalent forces aligns the molecules of macrocycles 1 and 2 into tubular stacks with cylindrical inner pores that, upon binding rod-like guests, lead to tight, discrete, and well-ordered tubular assemblies that are unprecedented in water.
Compound for targeted degradation of ALK, c-Met and ROS1 proteins, and preparation method thereof
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Paragraph 0115-0119, (2020/07/07)
The invention provides a novel compound for targeted degradation of ALK, c-Met and ROS1 proteins, wherein the compound is represented by a formula A, is formed by linking an ubiquitin ligase E3 recognition ligand and an ALK, c-Met and ROS1 protein inhibitor compound through a linking arm, and can selectively induce degradation of ALK, c-Met and ROS1 proteins and mutant proteins of the ALK, c-Met and ROS1 proteins. According to the invention, a bifunctional small molecule is obtained; and in-vitro anti-tumor activity data of the compound show that the compound has high-efficiency anti-tumor activity on conventional tumor cells, has strong inhibition activity on mutant cell strains (BaF3/EML4-ALKG1202R, BaF3/EML4-ALKL1196M and BaF3-TEL-ALK-C1156Y) causing the drug resistance, provides a effective antitumor drug for clinical application, has great application value, brings good news for tumor treatment, especially for some drug-resistant patients, and has important social benefits.
