85607-79-0Relevant articles and documents
COMPOUNDS AND THEIR USES AS MIF INHIBITORS
-
Paragraph 0191, (2022/01/08)
The present invention provides compounds of Formula I which can be used as macrophage migration inhibitory factor (MIF) inhibitors; methods for the production of the compounds of the invention; pharmaceutical compositions comprising the compounds of the i
Synthesis of p-O-Alkyl Salicylanilide Derivatives as Novel EGFR Inhibitors
Zhang, Li,Hou, Lin,Sun, Wenyan,Yu, Zidong,Wang, Jibo,Gao, Hua,Yang, Guiming
, p. 37 - 42 (2016/02/23)
(Table Presented) Epidermal growth factor receptor (EGFR), a validated target for anticancer drugs, plays a critical role in tumorigenesis and tumor development. A series of p-O-alkyl salicylanilide derivatives were designed and synthesized as novel EGFR inhibitors using a salicylic acid scaffold. A simulated six-membered ring strategy formed through intramolecular hydrogen bonds was employed to mimic the planar quinazoline of the EGFR antagonist, gefitinib. The derived compounds with hydroxyl at the ortho position were more potent than ones with methoxyl group. In particular, compounds 5d and 5b displayed significant EGFR inhibitory (IC50 values = 0.30 and 0.45 μM, respectively) activity as well as potent antiproliferative activity in A431 and HCT-116 tumor cells. These salicylanilides could be considered as promising lead compounds for developing novel EGFR inhibitors.
Compounds
-
Page/Page column 40, (2008/06/13)
This invention relates to nicotinamide derivatives of general formula (I): in which R1, Z and R2 have the meanings defined herein, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of such derivatives.
