153813-81-1Relevant articles and documents
Carboline derivative/analogue as well as preparation method and application thereof
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Paragraph 0219-0222, (2020/07/13)
The invention belongs to the field of chemical medicines, and provides a compound shown as a formula I or pharmaceutically acceptable salt thereof. The invention also provides analogues of the compound as shown in the formula I in the specification. Biological experiments show that the compound disclosed by the invention has anti-tumor activity and serves as a good tubulin inhibitor; the compound91b has excellent antitumor activity, can effectively promote degradation of tubulin; drug resistance caused by overexpression of beta-tubulin III and P-gp can be eliminated, and a new choice is provided for clinical medication.
HYPOXIA-INDUCIBLE FACTOR 1 (HIF-1) INHIBITORS
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Page/Page column 43, (2016/12/12)
Embodiments of small molecule inhibitors of hypoxia inducible factor 1 (HIF-1) and pharmaceutical compositions thereof are disclosed. The disclosed compounds suppress HIF-1 activity by inhibiting the interaction between the HIF- 1 α subunit and transcriptional co-activator protein p300. Embodiments of methods for making and using the small molecule inhibitors are also disclosed.
An straightforward entry to new pyrazolo-fused dibenzo[1,4]diazepines
Hernandez, Susana,Moreno, Isabel,Sanmartin, Raul,Teresa Herrero, Maria,Dominguez, Esther
supporting information; experimental part, p. 2251 - 2257 (2011/04/26)
A series of novel pyrazolodibenzo[1,4]diazepines has been synthesized with good overall yields. The diarylpyrazole intermediates, with structure similarity to biologically relevant compounds such as currently marketed drugs like rimonabant or celecoxib, were prepared by a tandem sequence amine-exchange/ heterocyclization starting from readily available enaminones and arylhydrazines. The key step of this efficient methodology was Caryl-N bond construction, accomplished by a palladium-catalyzed intramolecular N-arylation reaction, which was conducted in both homogeneous and polymer-supported versions. Reaction scope of such protocols and recycling of the heterogeneous catalyst were also examined.