87551-45-9Relevant articles and documents
[1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINES
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Page/Page column 347-348, (2021/02/19)
The present invention covers [1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds of general formula (I) in which R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients.
Structure-activity relationship studies and biological characterization of human NAD+-dependent 15-hydroxyprostaglandin dehydrogenase inhibitors
Duveau, Damien Y.,Yasgar, Adam,Wang, Yuhong,Hu, Xin,Kouznetsova, Jennifer,Brimacombe, Kyle R.,Jadhav, Ajit,Simeonov, Anton,Thomas, Craig J.,Maloney, David J.
supporting information, p. 630 - 635 (2014/01/23)
The structure-activity relationship (SAR) study of two chemotypes identified as inhibitors of the human NAD+-dependent 15-hydroxyprostaglandin dehydrogenase (HPGD, 15-PGDH) was conducted. Top compounds from both series displayed potent inhibition (IC50 2 production in A549 lung cancer and LNCaP prostate cancer cells.