Qin, Mingze; Meng, Yangyang; Yang, Haoshen; Liu, Lei; Zhang, Haotian; Wang, Simeng; Liu, Chunyang; Wu, Xia; Wu, Di; Tian, Ye; Hou, Yunlei; Zhao, Yanfang; Liu, Yajing; Xu, Congjun; Wang, Lihui published their research in Journal of Medicinal Chemistry in 2021. The article was titled 《Discovery of 4-Arylindolines Containing a Thiazole Moiety as Potential Antitumor Agents Inhibiting the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction》.Category: alcohols-buliding-blocks The article contains the following contents:
Through specific structural modification of a 4-phenylindoline precursor, new 4-arylindolines containing a thiazole moiety were developed and found to be promising modulators of the programmed cell death-1 (PD-1)/programmed cell death-ligand 1 (PD-L1) axis. Compound A30(I) exhibited outstanding biochem. activity, with an IC50 of 11.2 nM in a homogeneous time-resolved fluorescence assay. In the cell-based assay, A30 significantly promoted IFN-γ secretion and rescued T-cell proliferation, which were inhibited by PD-1 activation. Furthermore, A30 showed favorable in vivo antitumor activity in a mouse 4T1 breast carcinoma model. Moreover, in mouse CT26 colon carcinoma models, A30 potently suppressed the growth of CT26/PD-L1 tumor but did not obviously affect the growth of CT26/vector tumor. The results of flow cytometry anal. indicated that A30 inhibited tumor growth by activating the immune microenvironment. We concluded that A30 is a new starting point for further development of PD-1/PD-L1 interaction inhibitors as antitumor agents. The experimental part of the paper was very detailed, including the reaction process of trans-4-Aminocyclohexanol(cas: 27489-62-9Category: alcohols-buliding-blocks)
trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Left-handed and right-handed forms (mirror-image configurations, known as optical isomers or enantiomers) are possible when all the substituents on the central nitrogen atom are different (i.e., the nitrogen is chiral). With amines, there is extremely rapid inversion in which the two configurations are interconverted.Category: alcohols-buliding-blocks
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts