- Fluorine-substituted bimolecular carbazole derivative as well as preparation method and application thereof
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The invention discloses a fluorine-substituted bimolecular carbazole derivative represented by a formula (I) or pharmaceutically acceptable salt thereof. R1, R2, R3, R4 and R5 are defined in the specification. The fluorine-substituted bimolecular carbazole derivative or the pharmaceutically acceptable salt thereof provided by the invention can be used for preparing a DNA methyltransferase inhibitor or a histone demethylase inhibitor, and in-vitro cancer cell anti-proliferation tests prove that the fluorine-substituted bimolecular carbazole derivative has anti-proliferation activity on cancer cells.
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- Fluorine-substituted monocarbazole derivative as well as preparation method and application thereof (by machine translation)
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The invention belongs to the field of pharmaceutical chemistry, and relates to a fluorine-substituted monocarbazole derivative which is one or more of compounds represented by formula (I) and formula (II) or a pharmaceutically acceptable soluble salt formed by a compound represented by formula (II). The fluorine-substituted monocarbazole derivatives obtained in the application can be used for preparing DNA methyltransferase inhibitors or histone demethylase inhibitors. The fluorine-substituted monocarbazole derivative has an inhibitory effect on the proliferation of cancer cells and can be used for preparing medicaments for treating and/or preventing cancer. An in-vitro cancer cell proliferation inhibition test shows that the fluorine-substituted monocarbazole compound obtained by the invention shows anti-proliferation activity against human lung cancer cells (A549), human colon cancer cells (HCTCTCT116), human gastric cancer cells (MNK NK NK-45), human liver cancer cells (HepepepG2), RPMI PMI PMI PMI PMI PMI and Karpppp289. (by machine translation)
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Paragraph 0211
(2020/06/20)
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- COMPOUNDS THAT INHIBIT MCL-1 PROTEIN
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Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula (I), or a stereoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.
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Page/Page column 757
(2018/10/25)
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- Carbostyril carboxylic compounds and intermediates, preparation method and application thereof
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The invention discloses carbostyril carboxylic compounds and hydrochlorides thereof and also discloses a preparation method of the compounds and the hydrochlorides thereof as well as an application of the compounds and the hydrochlorides thereof in preparing gram-positive bacterium-preventing or gram-negative bacterium-preventing drugs. Moreover, the invention discloses intermediates for preparing the compounds and a preparation method of the intermediates.
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- General Procedures for the Lithiation/Trapping of N-Boc Piperazines
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To provide α-substituted piperazines for early stage medicinal chemistry studies, a simple, general synthetic approach is required. Here, we report the development of two general and simple procedures for the racemic lithiation/trapping of N-Boc piperazin
- Firth, James D.,O'Brien, Peter,Ferris, Leigh
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p. 7023 - 7031
(2017/07/17)
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- Discovery of novel N-aryl piperazine CXCR4 antagonists
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A novel series of CXCR4 antagonists with substituted piperazines as benzimidazole replacements is described. These compounds showed micromolar to nanomolar potency in CXCR4-mediated functional and HIV assays, namely inhibition of X4 HIV-1IIIB virus in MAGI-CCR5/CXCR4 cells and inhibition of SDF-1 induced calcium release in Chem-1 cells. Preliminary SAR investigations led to the identification of a series of N-aryl piperazines as the most potent compounds. Results show SAR that indicates type and position of the aromatic ring, as well as type of linker and stereochemistry are significant for activity. Profiling of several lead compounds showed that one (49b) reduced susceptibility towards CYP450 and hERG, and the best overall profile when considering both SDF-1 and HIV potencies (6-20 nM).
- Zhao, Huanyu,Prosser, Anthony R.,Liotta, Dennis C.,Wilson, Lawrence J.
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p. 4950 - 4955
(2015/10/28)
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- Discovery of novel leukotriene A4 hydrolase inhibitors based on piperidine and piperazine scaffolds
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Novel piperidine and piperazine derivatives have been designed and tested as inhibitors of LTA4 hydrolase (LTA4H). Most potent compounds showed good potency in both enzymatic and functional human whole blood assay. Crystallography studies further confirmed observed structure-activity relationship and LTA4H binding mode for analogs from the piperidine series.
- Sandanayaka, Vincent,Mamat, Bjorn,Bhagat, Nikhil,Bedell, Louis,Halldorsdottir, Gudrun,Sigthorsdottir, Heida,Andrésson, Thorkell,Kiselyov, Alex,Gurney, Mark,Singh, Jasbir
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scheme or table
p. 2851 - 2854
(2010/08/06)
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- Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 5: 2′-Substituted 6-nitroquipazines
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Five C2′-substituted 6-nitroquipazine (6-NQ) derivatives were prepared and evaluated in terms of their biological abilities (Ki) to displace [3H]citalopram binding to serotonin transporter. The relationship between their structure an
- Lee, Jae Hak,Choi, Yong Hyun,Lim, Yoo Jin,Lee, Byoung Se,Chi, Dae Yoon,Jin, Changbae
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p. 3499 - 3504
(2008/02/07)
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