Chenyu Tian

TL;DR: A comprehensive review of small-molecule targeted anti-cancer drugs according to the target classification is conducted, which presents all the approved drugs as well as important drug candidates in clinical trials for each target, and discusses the current challenges.

TL;DR: In this article , a series of potent α-ketoamide-containing Mpro inhibitors were obtained using the Ugi four-component reaction and the prioritized compound, Y180, showed an IC50 of 8.1 nM against SARS-CoV-2 Mpro and had oral bioavailability of 92.9%, 31.9% and 85.7% in mice, rats and dogs, respectively.

TL;DR: Among all the obtained dual inhibitors, 1-(3-chloro-4-fluorophenyl)-6-fluoro-1H-naphtho[2,3-d]triazole-4,9-dione (38) displayed the most potent IDO1 and TDO inhibitory activities with IC50 values, and could be a good lead compound for cancer immunotherapy and deserving further investigation.

TL;DR: The structural optimization and structure-activity relationship studies of 6,6-dimethyl-4-(phenylamino)-6H-pyrimido[5,4-b][1,4]oxazin-7(8H)-one derivatives as a new class of pan-Trk inhibitors are reported to show good kinase selectivity and could be a promising lead compound for drug discovery targeting Trks.

TL;DR: In in vivo models of PDAC xenografts (Aspc‐1 and Bxpc‐3), LY‐1816 showed more potent antitumor activity than dasatinib and gemcitabine and provided effective support for the subsequent clinical evaluation of LY-1816 in the treatment ofPDAC.