90213-67-5Relevant academic research and scientific papers
Synthesis and fluorescent properties of N(9)-alkylated 2-amino-6-triazolylpurines and 7-deazapurines
?i?u?ins, Andrejs,Bucevi?ius, Jonas,Tseng, Yu-Ting,Novosjolova, Irina,Traskovskis, Kaspars,Bizdēna, ērika,Chang, Huan-Tsung,Tumkevi?ius, Sigitas,Turks, Māris
, p. 474 - 489 (2019)
The synthesis of novel fluorescent N(9)-alkylated 2-amino-6-triazolylpurine and 7-deazapurine derivatives is described. A new C(2)-regioselectivity in the nucleophilic aromatic substitution reactions of 9-alkylated-2,6-diazidopurines and 7-deazapurines wi
NOVEL SULFONAMIDE DERIVATIVE WITH FUSED PYRIMIDINE SKELETON, HAVING EPIDERMAL GROWTH FACTOR RECEPTOR MUTATION INHIBITORY EFFECT
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Sheet 0105; 0106, (2021/07/02)
The present invention relates to a novel fused pyrimidine based sulfonamide derivative represented by Formula I, a solvate thereof, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition including the same as an active ingredient. The novel fused pyrimidine based sulfonamide derivative of the present invention can effectively suppress the growth of cancer cells and resistance to drugs, which are induced by mutations in the tyrosine kinase domain of epidermal growth factor receptors, or the growth of cancer cells having such resistance.
Design, synthesis and biological evaluation of sphingosine-1-phosphate receptor 2 antagonists as potent 5-FU-resistance reversal agents for the treatment of colorectal cancer
Cui, Shuxiang,Guo, Zhikun,Han, Gaitian,Liu, Shuai,Liu, Xiaochun,Luo, Dongdong,Lv, Yan,Qu, Xianjun,Tian, Xiaochen,Wan, Shengbiao,Wang, Wenyu,Yang, Shuang,Zhang, Yuhang
, (2021/08/20)
5-Fluorouracil (5-FU) and its prodrugs are the essential clinical drugs for colorectal cancer (CRC) treatment. However, the drug resistance of 5-FU has caused high mortality of CRC patients. Thus, it is urgent to develop reversal agents of 5-FU resistance. Sphingosine-1-phosphate receptor 2 (S1PR2) was proved to be a potential target for reversing 5-FU resistance, but the activity of known S1PR2 antagonists JTE-013 were weak in 5-FU-resistant cell lines. To develop more potent S1PR2 antagonists to treat 5-FU-resistant cancer, a series of JTE-013 derivatives were designed and synthesized. The most promising compound 40 could markedly reverse the resistance in 5-FU-resistant HCT116 cells and 5-FU-resistant SW620 cells via inhibiting the expression of dihydropyrimidine dehydrogenase (DPD). The key was that compound 40 with improved pharmacokinetic properties significantly increased the inhibitory rate of 5-FU in the SW620/5-FU cells xenograft model with no observable toxicity by inhibiting the expression of DPD in tumor and liver tissues. Altogether, these results suggest that compound 40 may be a promising drug candidate to reverse 5-FU resistance in the treatment of CRC.
Design and Discovery of an Orally Efficacious Spiroindolinone-Based Tankyrase Inhibitor for the Treatment of Colon Cancer
Shirai, Fumiyuki,Mizutani, Anna,Yashiroda, Yoko,Tsumura, Takeshi,Kano, Yuko,Muramatsu, Yukiko,Chikada, Tsubasa,Yuki, Hitomi,Niwa, Hideaki,Sato, Shin,Washizuka, Kenichi,Koda, Yasuko,Mazaki, Yui,Jang, Myung-Kyu,Yoshida, Haruka,Nagamori, Akiko,Okue, Masayuki,Watanabe, Takashi,Kitamura, Kouichi,Shitara, Eiki,Honma, Teruki,Umehara, Takashi,Shirouzu, Mikako,Fukami, Takehiro,Seimiya, Hiroyuki,Yoshida, Minoru,Koyama, Hiroo
supporting information, p. 4183 - 4204 (2020/05/20)
Tankyrases (TNKS/TNKS2) belong to the poly(ADP-ribose) polymerase family. Inhibition of their enzymatic activities attenuates the Wnt/β-catenin signaling, which plays an important role in cancer pathogenesis. We previously reported the discovery of RK-287107, a spiroindoline-based, highly selective, potent tankyrase inhibitor. Herein we describe the optimization process of RK-287107 leading to RK-582, which exhibits a markedly improved robust tumor growth inhibition in a COLO-320DM mouse xenograft model when orally administered. In addition to the dose-dependent elevation and attenuation of the levels of biomarkers AXIN2 and β-catenin, respectively, results of the TCF reporter and cell proliferation studies on COLO-320DM are discussed.
INHIBITORS OF INFLUENZA VIRUS REPLICATION, APPLICATION METHODS AND USES THEREOF
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Paragraph 00262, (2018/03/09)
A class of compounds as inhibitors of influenza virus replication, preparation methods thereof, pharmaceutical compositions containing these compounds, and uses of these compounds and pharmaceutical compositions thereof in the treatment of influenza.
Influenza virus replication inhibitor and application thereof
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Paragraph 0554; 0556; 0557; 0920; 0922; 0923, (2018/07/30)
The invention relates to an influenza virus replication inhibitor and application thereof, and particularly relates to a compound serving as an influenza virus replication inhibitor, a preparation method thereof, a pharmaceutical composition containing the compound, and application of the compound and the pharmaceutical composition to influenza treatment.
INHIBITORS OF INFLUENZA VIRUS REPLICATION AND USES THEREOF
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Paragraph 00273; 00370, (2018/07/31)
Provided herein is inhibitors of influenza virus replication and uses thereof. Specifically, provided herein a novel class of compounds as inhibitors of influenza virus replication, preparation methods thereof, pharmaceutical compositions containing these compounds, and uses of these compounds and pharmaceutical compositions thereof in the treatment of influenza.
INHIBITORS OF INFLUENZA VIRUS REPLICATION AND USES THEREOF
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Paragraph 00243, (2018/09/21)
The invention provides a novel class of compounds as inhibitors of influenza virus replication, preparation methods thereof, pharmaceutical compositions containing these compounds, and uses of these compounds and pharmaceutical compositions thereof in the treatment of influenza.
SUBSTITUTED BICYCLIC PYRIMIDINE-BASED COMPOUNDS AND COMPOSITIONS AND USES THEREOF
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Paragraph 00235; 00236, (2018/08/20)
Novel C-2-substituted bicyclic compounds of Formula I have been prepared and found to be useful as potent inhibitors of hGGPPS by inhibiting geranylgeranylation of proteins and inhibiting the biosynthesis of GGPP. The application is directed to these compounds, to compositions comprising these compounds, and to their use, in particular as medicaments for use in the treatment of cancer and other conditions which are treatable by inhibiting human geranylgeranylation pyrophosphate hGGPPS activity.
INHIBITORS OF INFLUENZA VIRUS REPLICATION AND USES THEREOF
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Paragraph 00339, (2018/07/05)
The invention provides a class of compounds as inhibitors of influenza virus replication, preparation methods thereof, pharmaceutical compositions containing these compounds, and uses of these compounds and pharmaceutical compositions thereof in the treatment of influenza.
