75665-88-2Relevant articles and documents
Heterocyclic compound, preparation method and application thereof
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Paragraph 0161; 0164-0165, (2020/07/02)
The invention relates to a heterocyclic compound in the technical field of medicines. The compound is represented by a structural general formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, X, Y, Z, Cy1, Cy2, m, n and t have the meanings given in the specification; in addition, the invention also discloses an application of the compound and the pharmaceuticallyacceptable salt thereof in preparation of drugs for treating diseases caused by abnormal high expression of tyrosine kinase, especially application in preparation of drugs for treating and preventingcancers.
Ipomoeassin F Binds Sec61α to Inhibit Protein Translocation
Zong, Guanghui,Hu, Zhijian,O'Keefe, Sarah,Tranter, Dale,Iannotti, Michael J.,Baron, Ludivine,Hall, Belinda,Corfield, Katherine,Paatero, Anja O.,Henderson, Mark J.,Roboti, Peristera,Zhou, Jianhong,Sun, Xianwei,Govindarajan, Mugunthan,Rohde, Jason M.,Blanchard, Nicolas,Simmonds, Rachel,Inglese, James,Du, Yuchun,Demangel, Caroline,High, Stephen,Paavilainen, Ville O.,Shi, Wei Q.
, p. 8450 - 8461 (2019/06/04)
Ipomoeassin F is a potent natural cytotoxin that inhibits growth of many tumor cell lines with single-digit nanomolar potency. However, its biological and pharmacological properties have remained largely unexplored. Building upon our earlier achievements
CARBAMATE AND UREA COMPOUNDS AS MULTIKINASE INHIBITORS
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Paragraph 069, (2019/07/13)
The present disclosure describes carbamate and urea compounds as novel multikinase inhibitors and methods for preparing them. The pharmaceutical compositions comprising such multikinase inhibitors and methods of using them for treating cancer, infectious diseases, and other disorders associated with kinases are also described.
Molecularly imprinted artificial esterases with highly specific active sites and precisely installed catalytic groups
Hu, Lan,Zhao, Yan
, p. 5580 - 5584 (2018/08/17)
A difficult challenge in synthetic enzymes is the creation of substrate-selective active sites with accurately positioned catalytic groups. Covalent molecular imprinting in cross-linked micelles afforded such active sites in protein-sized, water-soluble nanoparticle catalysts. Our method allowed a systematic tuning of the distance of the catalytic group to the bound substrate. The catalysts displayed enzyme-like kinetics and easily distinguished substrates with subtle structural differences.
Design and Construction of a Smart Targeting Drug Delivery System Based on Phototriggered Competition of Host–Guest Interaction
Zhao, Dan,Yi, Xiaoqing,Yuan, Gongdao,Zhuo, Renxi,Li, Feng
, (2017/09/23)
A smart targeting drug delivery nanocarrier is successfully constructed based on phototriggered competition of host–guest interaction. The targeting motif, i.e., biotin is first concealed by β-cyclodextrin (β-CD) via host–guest interaction. When the nanoparticles are exposed to UV light, the cleavage of photosensitive groups results in the exposure of adamantane (Ad) groups initially located in the interior of nanoassemblies, and β-CDs capped on biotin ligands can be replaced by Ad because of the higher binding constant between Ad and β-CD than that between biotin and β-CD. The competition of host–guest interaction leads to the recovery of targeting capacity of biotin ligands on the nanocarriers. By virtue of photoregulation, the nanocarriers exhibit controllable ligand-receptor recognition, which is proved by flow cytometry, laser confocal microscopy, and cytotoxicity assay. This strategy has a potential to improve the selectivity and safety of targeting drug delivery systems.
Quinoline or quinazoline derivatives as well as preparation method and application thereof
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Paragraph 0229; 0230, (2017/04/11)
The invention relates to quinoline or quinazoline derivatives as well as a preparation method and an application thereof, namely, the quinoline or quinazoline derivatives shown as the formula I as well as pharmaceutically acceptable salts and hydrates or prodrugs of the quinoline or quinazoline derivatives. The structure is shown in the specification, wherein A1, A2, R1, R2, R3, R4, R5, R6, X, Y, Z, M, W, Cy1, Cy2, m and n are defined in the specification. The invention further relates to the function of the compounds in the general formula I for inhibiting MET kinase and the application of the compounds as well as the pharmaceutically acceptable salts and hydrates of the compounds in preparation of drugs for treating diseases caused by abnormal high expression of the MET kinase, in particular to the application in preparation of drugs for treating and preventing cancer.
A alkyne generation quinoline derivatives and its preparation and use
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Paragraph 0114; 0115, (2017/08/25)
The invention discloses alkynylquinoline derivatives, and a preparation method and application thereof. The acetylenoquinoline derivatives are alkynylquinoline compounds as shown in a general formula I which is described in the specification and pharmaceutically acceptable salts, hydrates, solvates and prodrugs thereof. The invention also provides the preparation method for the derivatives and relates to inhibition activity of the compounds as shown in the formula I to a variety of protein tyrosine kinases (e.g. C-Met and VEGFR). Thus, the compounds can be used as anticancer drugs for treatment of human cancers.
Substituent effects at the benzyl position and aromatic ring of silane-coupling agents containing 2-nitrobenzyl esters on photosensitivity and hydrophobic surface of a self-assembled monolayer (SAM)
Konishi, Tsubasa,Hashimoto, Teppei,Sato, Naoya,Nakajima, Kazuki,Yamaguchi, Kazuo
, p. 125 - 134 (2016/01/27)
Silane-coupling agents with 2-nitrobenzyl esters containing alkyl substituents at the benzyl position and alkoxy and/or fluoroalkoxy groups of the aromatic ring were synthesized to prepare a self-assembled monolayer (SAM) on quartz glass, silicon wafer and thermally oxidized silicon wafer. The resulting photosensitive SAMs before and after photoirradiation were characterized by contact angle measurement, UV spectroscopy, X-ray photoelectron spectroscopy (XPS), and X-ray reflectivity (XRR). Photosensitivity of the SAM was influenced by substituents at the benzyl position and aromatic ring as well as the irradiation conditions in air or solution and substrates employed. Silane-coupling agents with bulky substituent at the benzyl position and double fluoroalkoxy chains are preferable in terms of the photosensitivity and hydrophobic surface.
FLUORINE-CONTAINING COMPOUND, PATTERN FORMING SUBSTRATE, PHOTODEGRADABLE COUPLING AGENT, PATTERN FORMING METHOD, COMPOUND, AND ORGANIC THIN FILM TRANSISTOR
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, (2016/10/08)
PROBLEM TO BE SOLVED: To provide a compound that has a big difference in contact angle before and after light irradiation and is useful as a coupling agent, and an organic thin film transistor prepared by using the compound. SOLUTION: A fluorine-containin
Synthesis and in vitro characterization of cinnoline and benzimidazole analogues as phosphodiesterase 10A inhibitors
Yang, Hao,Murigi, Francis N.,Wang, Zhijian,Li, Junfeng,Jin, Hongjun,Tu, Zhude
supporting information, p. 919 - 924 (2015/02/19)
Fifteen cinnoline analogues and six benzimidazole phosphodiesterase 10A (PDE10A) inhibitors were synthesized as potential PET radiopharmaceuticals and their in vitro activity as PDE10A inhibitors was determined. Nine out of twenty-one compounds were potent inhibitors of PDE10A with IC50 values ranging from 1.5 to 18.6 nM. Notably, the IC50 values of compounds 26a, 26b, and 33c were 1.52 ± 0.18, 2.86 ± 0.10, and 3.73 ± 0.60 nM, respectively; these three compounds also showed high in vitro selectivity (>1000-fold) for PDE10A over PDE 3A/3B, PDE4A/4B. The high potency and selectivity of these three compounds suggests that they could be radiolabeled with PET radionuclides for further evaluation of their in vivo pharmacological behavior and ability to quantify PDE10A in the brain.