46065-16-1Relevant articles and documents
PHARMACEUTICAL COMPOSITIONS COMPRISING DICARBOXYLIC ACIDS AND THEIR THERAPEUTIC APPLICATIONS
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Paragraph 00275, (2019/08/20)
Provided herein are pharmaceutical compositions, each comprising a dicarboxylic acid, for example, a compound of Formula I, or an enantiomer, a mixture of enantiomers, a mixture of two or more diastereomers, a tautomer, a mixture of two or more tautomers,
Novel bivalent securinine mimetics as topoisomerase I inhibitors
Hou, Wen,Lin, Hui,Wang, Zhen-Ya,Banwell, Martin G.,Zeng, Ting,Sun, Ping-Hua,Lin, Jing,Chen, Wei-Min
, p. 320 - 328 (2017/03/08)
A series of novel bivalent securinine mimetics incorporating different linkers between C-15 and C-15′ were synthesized and their topoisomerase I (Topo I) inhibitory activities evaluated. It was thus revealed that mimetic R2 incorporating a rigid m-substituted benzene linker exhibits Topo I inhibitory activity three times that of parent securinine. Comprehensive structure-activity relationship analyses in combination with docking studies were used to rationalize the potent activity of these bivalent mimetics. Mechanistic studies served to confirm the deductions arising from docking studies that the active bivalent mimetics not only inhibited complexation between Topo I and DNA but also stabilized the Topo I-DNA complex itself.
COMPOUNDS AND THEIR METHODS OF USE
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Paragraph 0324; 0335; 0336, (2014/05/25)
Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.
