- Amide compounds for regulating WNT signal channel and application of compounds
-
The invention belongs to the technical field of medicine, and particularly relates to amide compounds for regulating a WNT signal channel and an application of the compounds. The compounds have a structure represented by a general formula I shown in the description.
- -
-
Paragraph 0154; 0155
(2019/07/11)
-
- Discovery and structure-activity relationship study of phthalimide-phenylpyridine conjugate as inhibitor of Wnt pathway
-
Aberrant Wnt signaling has been implicated in a variety of disease. Inhibition of the Wnt pathway is an attractive approach for developing new therapeutics for the treatment of various types of fibrosis and cancers. We have discovered the phthalimide-phenylpyridine conjugate as a novel hit compound for the Wnt pathway inhibitors from cellular screening. The structure-activity relationship of these compounds suggested both of the substituent group on the phthalimide fragment and the structure of the linker were critical to the inhibitory activity. The most potent compound was about 10-folds more potent than the hit compound, with IC50 value of 0.28 ± 0.01 μM.
- Wu, Hongna,Wu, Jun,Zhang, Wenxuan,Li, Zhongwen,Fang, Jinhui,Lian, Xu,Qin, Tong,Hao, Jie,Zhou, Qi,Wu, Song
-
supporting information
p. 870 - 872
(2019/02/16)
-
- Anticonvulsant and neurotoxicity evaluation of new bromophthalimido-butyryl hydrazones
-
A new series of N-aryl/alkylidene-4-(5-bromo-1,3-dioxo-1,3-dihydro-2H- isoindol-2-yl) butanoyl hydrazones (4a-I) were synthesized and evaluated for their anticonvulsant activity in MES test according to the protocols of Antiepileptic Drug Development (ADD
- Kamal, Mehnaz,Khan, Suroor A.,Jawaid, Talha
-
experimental part
p. 321 - 324
(2012/01/03)
-
- Anticonvulsant and neurotoxicity evaluation of new bromophthalimidobutyryl amide derivatives
-
A series of 4-(5-bromo-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-butyryl N-(substituted phenyl) amides (3a-l) were synthesized and evaluated for their anticonvulsant activity in MES test according to the protocols of Antiepileptic Drug Development (ADD) programme of National Institutes of Health (NIH, Bethesda, USA).The most active compounds of the series were 3a, 3c, 3d, 3f, 3g, 3i and 3k at the dose of 30 mg/kg (i.p.) 0.5 h and 4 h after administration. In neurotoxic screen (NT), 3d, 3i and 3k were less toxic when compared with the other compounds.
- Khan, Suroor A.,Siddiqui, Nadeem,Kamal, Mehnaz,Alam, Ozair,Jawaid, Talha
-
experimental part
p. 65 - 68
(2009/06/06)
-