3153-32-0Relevant academic research and scientific papers
Lysine derivative histone deacetylase inhibitor, synthesis and application
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Paragraph 0040; 0041; 0042, (2018/04/02)
The invention discloses a lysine derivative histone deacetylase inhibitor. The inhibitor has high selectivity, can be used for Sirtuin mechanism inhibitor antitumor drugs with strong Sirtuin selectivity, high efficiency and low toxicity, has easily available raw materials, and is low in cost.
The mimics of Nε-acyl-lysine derived from cysteine as sirtuin inhibitors
Wang, Chun,Wang, Fang,Chen, Xiaoxue,Zou, Yefang,Zhu, Hong,Zhao, Qingjie,Shen, Jingshan,Li, Yan,Li, Yongjun,He, Bin
supporting information, p. 2375 - 2378 (2018/06/20)
Sirtuin inhibitors as physiological research tools and therapeutic potentials have caught many attentions in last decades. The mimics of acyl lysine have been approved to be a very efficient strategy for development of mechanism-based sirtuin inhibitors. In current study, a novel scaffold of L-S-(3-carboxamidopropyl) cysteine (L-CAPC) has been exploited for design and synthesis of sirtuin inhibitors. As a result, the mimics of Nε-acyl-lysine derived from cysteine including small molecules (5a–m) and peptides (9a–m) have been synthesized. Among these, the peptides 9g and 9h were found to be the most inhibitory potency and selectivity against SIRT2.
NOVEL SUBSTITUTED ARYL DERIVATIVES, THEIR PROCESS OF PREPARATION AND THEIR THERAPEUTICAL USES AS ANTI-HIV AGENTS
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Page/Page column 86, (2010/06/22)
The present invention concerns novel substituted aryl derivatives, their process of preparation and their use for inhibiting virus replication and for treating viral diseases or disorders such as HIV and/or HCV infection.
Syntheses of tetrahydrothiophenes and tetrahydrofurans and studies of their derivatives as melanocortin-4 receptor ligands
Tran, Joe A.,Chen, Caroline W.,Tucci, Fabio C.,Jiang, Wanlong,Fleck, Beth A.,Chen, Chen
, p. 1124 - 1130 (2008/09/18)
Piperazinebenzylamine derivatives from trans-4-(4-chlorophenyl)tetrahydrothiophene-3-carboxylic acid 6 and its S-oxide 7 and sulfone 8, and the tetrahydrofuran 9 and its two regioisomers 11 and 13 were synthesized and studied for their binding affinities at the human melanocortin-4 receptor. These five-membered ring constrained compounds possessed similar or lower potency compared to the acyclic analogs.
ANTI-CANCER AGENTS
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Page/Page column 60, (2010/02/11)
The present invention provides compounds having the strucutural formula (I) and methods for the treatment of cancer using compounds of formula (I).
Synthesis and structure-activity relationships of pyrazine-pyridine biheteroaryls as novel, potent, and selective vascular endothelial growth factor receptor-2 inhibitors
Kuo, Gee-Hong,Prouty, Catherine,Wang, Aihua,Emanuel, Stuart,DeAngelis, Alan,Zhang, Yan,Song, Fengbin,Beall, Lawrence,Connolly, Peter J.,Karnachi, Prahba,Chen, Xin,Gruninger, Robert H.,Sechler, Jan,Fuentes-Pesquera, Angel,Middleton, Steven A.,Jolliffe, Linda,Murray, William V.
, p. 4892 - 4909 (2007/10/03)
There is much evidence that direct inhibition of the kinase activity of vascular endothelial growth factor receptor-2 (VEGFR-2) will result in the reduction of angiogenesis and the suppression of tumor growth. Palladium-catalyzed C-C bond, C-N bond formation reactions were used to assemble various pyrazine-pyridine biheteroaryls as potent VEGFR-2 inhibitors. Among them, 4-{5-[6-(3-chloro-phenylamino)-pyrazin-2-yl]-pyridin-3-ylamino}-butan-1-ol (39) and N-{5-[6-(3-chloro-phenylamino)-pyrazin-2-yl]-pyridin-3-yl}-N′, N′-dimethyl-ethane-1,2-diamine (41) exhibited the highest kinase selectivity against fibroblast growth factor receptor kinase, platelet-derived growth factor receptor kinase, and glycogen synthase kinase-3. All of these compounds showed good cellular potency to inhibit VEGF-stimulated proliferation of human umbilical vein endothelial cells (HUVEC) but with modest effects on the unstimulated growth of HUVEC. The low inhibition of these compounds to the growth of tumor cell lines, such as HeLa, HCT-116, and A375 further confirms that these VEGFR-2 inhibitors are not cytotoxic agents. The in vivo antitumor activity of 39 and 41 were demonstrated in the A375 human melanoma xenograft nude mice model. Molecular modeling (QSAR analysis) was conducted in an attempt to rationalize the observed structure-activity relationship.
LIGANDS OF MELANOCORTIN RECEPTORS AND COMPOSITIONS AND METHODS RELATED THERETO
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Page/Page column 66, (2010/02/11)
Compounds which function as melanocortin receptor ligands and having utility in the treatment of melanocortin receptor-based disorders. The compounds have the following structure (I): (R4)s (R 2)n N~ X1-X2 (CR1aCRlb)q 1~ N R1-lm 1 O R3 (I) including stereoisomers, prodrugs, and pharmaceutically acceptable salts thereof, wherein m, n, q, s, R1, R1a, R1b, R2, R3, R4, X1 X2 and X3 are as defined herein. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof, are also disclosed.
Fluorescent probes for DNA detection by hybridization with improved sensitivity and low background
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, (2008/06/13)
Minor groove binder-oligonucleotide probes are provided along with methods for their use wherein the probes have an attached fluorophore which, in an unhybridized form exhibits very low background signal.
Antiproliferative and phenotype-transforming antitumor agents derived from cysteine
Glenn, Matthew P.,Kahnberg, Pia,Boyle, Glen M.,Hansford, Karl A.,Hans, Dhiraj,Martyn, Adam C.,Parsons, Peter G.,Fairlie, David P.
, p. 2984 - 2994 (2007/10/03)
Selective destruction of malignant tumor cells without damaging normal cells is an important goal for cancer chemotherapy in the 21st century. Differentiating agents that transform cancer cells to either a nonproliferating or normal phenotype could potent
Novel compounds and compositions for treating diseases asociated with protease activity
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, (2008/06/13)
Novel compounds, compositions and methods effective for the prevention and treatment of mast-cell mediated inflammatory disorders are described. The compounds, compositions and methods are effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis, as well as other types of immunomediated inflammatory disorders, such as rheumatoid arthritis, conjunctivitis and inflammatory bowel disease, various dermatological conditions, as well as certain viral conditions. The compounds comprise potent and selective inhibitors of the mast cell protease tryptase. The compositions for treating these conditions include oral, inhalant, topical and parenteral preparations as well as devices comprising such preparations.
