400720-72-1Relevant academic research and scientific papers
TRICYCLIC AKR1C3 DEPENDENT KARS INHIBITORS
-
Page/Page column 58; 80, (2021/01/29)
The present invention relates to novel tricyclic compounds that are AKR1C3 dependent KARS inhibitor, processes for their preparation, pharmaceutical compositions, and medicaments containing them, and their use in diseases and disorders mediated by an AKR1C3 dependent KARS inhibitor.
Design, synthesis, and biological evaluation of new diaminoquinazolines as β-catenin/Tcf4 pathway inhibitors
Mao, Yongjun,Lin, Nan,Tian, Wang,Han, Xiaofeng,Han, Xiaobing,Huang, Ziwei,An, Jing
experimental part, p. 1346 - 1359 (2012/04/04)
More than 50 new diaminoquinazoline derivatives have been synthesized and evaluated in a colon carcinoma cell growth inhibition assay using HCT116 and SW480 cells. Twenty compounds with good cell growth inhibitory activities (50 values 50 values of 1.5-2.5 μM for HCT116 cells with the luciferase reporter assay.
Synthesis and structural optimization of multiple H-bonding region of diarylalkyl (thio)amides as novel TRPV1 antagonists
Li, Fu-Nan,Kim, Nam-Jung,Chang, Dong-Jo,Jang, Jaebong,Jang, Hannah,Jung, Jong-Wha,Min, Kyung-Hoon,Jeong, Yeon-Su,Kim, Sun-Young,Park, Young-Ho,Kim, Hee-Doo,Park, Hyeung-Geun,Suh, Young-Ger
experimental part, p. 8149 - 8160 (2010/03/25)
Structural optimization of multiple H-bonding region and structure-activity relationship of diarylalkyl amides/thioamides as novel TRPV1 antagonists are described. In particular, we identified amide 34o and thioamides 35o and 35r, of which antagonistic activities were highly enhanced by an incorporation of cyano or vinyl-substituent to the multiple H-bonding region. They exhibited potent 45Ca2+ uptake inhibitions in rat DRG neuron with IC50s of 25, 32 and 28 nM, respectively.
