- Antitumor compound, synthesis method and applications thereof
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The invention belongs to the field of medicinal chemistry, and particularly relates to an antitumor compound, a synthesis method and applications thereof, wherein the compound has a structure represented by a general formula I or a general formula II, and
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Paragraph 0136-0140
(2020/05/01)
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- Acridinium-Based Photocatalysts: A Sustainable Option in Photoredox Catalysis
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The emergence of visible light photoredox catalysis has enabled the productive use of lower energy radiation, leading to highly selective reaction platforms. Polypyridyl complexes of iridium and ruthenium have served as popular photocatalysts in recent ye
- Joshi-Pangu, Amruta,Lévesque, Fran?ois,Roth, Hudson G.,Oliver, Steven F.,Campeau, Louis-Charles,Nicewicz, David,DiRocco, Daniel A.
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p. 7244 - 7249
(2016/08/30)
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- ACRIDINES AS INHIBITORS OF HASPIN AND DYRK KINASES
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The present disclosure is directed to compounds of Formula I: which are inhibitors of Haspin kinase and DYRK kinases. The compounds of the present disclosure, and compositions thereof, are useful in the treatment of disease related to Haspin kinase and DY
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Page/Page column 28; 29; 32
(2011/10/31)
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- Structure-activity relationship study of acridine analogs as haspin and DYRK2 kinase inhibitors
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Haspin is a serine/threonine kinase required for completion of normal mitosis that is highly expressed during cell proliferation, including in a number of neoplasms. Consequently, it has emerged as a potential therapeutic target in oncology. A high throughput screen of approximately 140,000 compounds identified an acridine analog as a potent haspin kinase inhibitor. Profiling against a panel of 270 kinases revealed that the compound also exhibited potent inhibitory activity for DYRK2, another serine/threonine kinase. An optimization study of the acridine series revealed that the structure-activity relationship (SAR) of the acridine series for haspin and DYRK2 inhibition had many similarities. However, several structural differences were noted that allowed generation of a potent haspin kinase inhibitor (33, IC50 50 400 nM) with a 5.4-fold selectivity over haspin was also identified.
- Cuny, Gregory D.,Robin, Maxime,Ulyanova, Natalia P.,Patnaik, Debasis,Pique, Valerie,Casano, Gilles,Liu, Ji-Feng,Lin, Xiangjie,Xian, Jun,Glicksman, Marcie A.,Stein, Ross L.,Higgins, Jonathan M.G.
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scheme or table
p. 3491 - 3494
(2010/08/21)
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- Photoswitchable macrocycles incorporating acridane moieties
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Novel crown ethers incorporating one to three 9-phenyl-acridinium units were synthesized in moderate yields. The acridinium units within the macrocycles were converted into the photoactive N-methyl-9-methoxy-9-phenyl-9,10- dihydroacridine (N-methyl-9-methoxy-9-phenylacridane) units. Georg Thieme Verlag Stuttgart.
- Orda-Zgadzaj, Marzena,Abraham, Werner
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p. 3345 - 3356
(2008/09/21)
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- Potential anticancer agents derived from acridine
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The compounds of the subject invention can be represented as follows: STR1 wherein each of R1, R2, R3, R4, are the same or different and are hydrogen (H), or a lower alkyl group of from about 1-4 carbon atoms, o
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