141761-82-2Relevant articles and documents
WDR5-MYC INHIBITORS
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Paragraph 00495; 00808; 001066; 001068, (2021/02/05)
Substituted N-phenyl sulfonamide compounds inhibit WDR5-MYC interactions, and the compounds and their pharmaceutical compositions are useful for treating disorders and conditions in a subject, such as cancer cell proliferation.
Benzoheterocycle-carboxamide-pyridone derivatives and preparation method and applications thereof
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Paragraph 0099; 0100; 0101; 0102, (2018/03/26)
The invention belongs to the field of chemical medicine preparation, and concretely relates to benzoheterocycle-carboxamide-pyridone derivatives, a preparation method and applications thereof. The invention provides the benzoheterocycle-carboxamide-pyridone derivatives, and a structure is represented by a formula I. The present invention also provides the preparation method and the applications ofthe above benzoheterocycle-carboxamide-pyridone derivatives. The benzoheterocycle-carboxamide-pyridone derivatives provided by the invention are novel compounds obtained on the basis of a large number of screening, inhibit EZH2 activity, and provide a novel selection for development and application of medicines for resisting tumors and autoimmune diseases.
Synthesis and pharmacology of 3,4-dihydro-3-oxo-1,4-benzoxazine-8-carboxamide derivatives, a new class of potent serotonin-3 (5-HT3) receptor antagonists
Kawakita,Kuroita,Yasumoto,Sano,Inaba,Fukuda,Tahara
, p. 624 - 630 (2007/10/02)
A series of 3,4-dihydro-3-oxo-1,4-benzoxazine-8-carboxamide derivatives was synthesized and evaluated for serotonin-3 (5-HT3) receptor antagonistic activity assessed by their ability to antagonize the von Bezold-Jarish (BJ) effect in rats. Derivatives bearing 1-azabicyclo[2.2.2]oct-3-yl moiety as a basic function attached to the carboxamide at position 8 showed more potent antagonistic activity than those bearing the other three basic moieties. Structure activity relationships of this series showed that methyl and chloro groups were more effective as substituents at positions 4 and 6, respectively. The representative compound 15 (Y-25130) in this series showed potent antagonistic activity on the BJ effect (ED50 = 1.3 μg/kg i.v.), high affinity for 5-HT3 receptor (K(i) = 2.9 nM) and complete protection against cisplatin-induced emesis in dogs at a dose of 0.1 mg/kg i.v.