873852-15-4Relevant academic research and scientific papers
The discovery of potent small molecule activators of human STING
Pryde, David C.,Middya, Sandip,Banerjee, Monali,Shrivastava, Ritesh,Basu, Sourav,Ghosh, Rajib,Yadav, Dharmendra B.,Surya, Arjun
supporting information, (2020/10/09)
The adaptor protein STING plays a major role in innate immune sensing of cytosolic nucleic acids, by triggering a robust interferon response. Despite the importance of this protein as a potential therapeutic target for serious unmet medical conditions inc
QUINAZOLINE HETEROCYCLIC COMPOUND AS EGFR KINASE INHIBITOR AND PREPARATION AND APPLICATION THEREOF
-
, (2018/01/19)
The present invention relates to an N-substituted-phenyl-5-substituted-alkoxy-2,3-dihydro-[1,4]dioxane[2,3-f]quinazolin-10-amine (I) or 4-substituted-arylamino-6-substituted-alkyl-6H-[1,4]oxazino[3,2-g]quinazoline-7(8H)-one (II) type compounds, a preparation method thereof and an application thereof as an inhibitor for epidermal growth factor receptor (EGFR) (comprising some mutant forms of EGFR) to treat cancer. These compounds and salts thereof can be used to treat or prevent various cancer diseases.
Novel morpholin-3-one fused quinazoline derivatives as EGFR tyrosine kinase inhibitors
Qin, Xuemei,Lv, Yongjuan,Liu, Peng,Li, Zhipeng,Hu, Liming,Zeng, Chengchu,Yang, Leifu
, p. 1571 - 1575 (2016/07/27)
A series of novel morpholin-3-one-fused quinazoline derivatives were designed, synthesized and evaluated as EGFR tyrosine kinase inhibitors. Nineteen compounds showed significant inhibitory activities against EGFRwtkinase (IC50?wt(IC50?=?53.1?nM). Compound a7 and a8 showed excellent inhibitory activities against mutant EGFRT790M/L858Rand strong antiproliferative activity against H358 and A549 cell lines. Finally, molecular docking studies were performed to predict the possible binding mode of the target compounds. It is believed that this work would be very useful for designing a new series of tyrosine kinase inhibitors targeting EGFR.
New herbicide models from benzoxazinones: Aromatic ring functionalization effects
Macias, Francisco A.,De Siqueira, Joao M.,Chinchilla, Nuria,Marin, David,Varela, Rosa M.,Molinillo, Jose M. G.
, p. 9843 - 9851 (2008/02/04)
The utility of benzoxazinones and some of their synthetic derivatives in the search for new leads for herbicide model development has been widely discussed. As the benzoxazinone skeleton contains three different potential areas for functionalization (C-2,
3-Aminobenzamide compounds and inhibitors of vanilloid receptor subtype 1 (VR1) activity
-
Page/Page column 25, (2010/10/19)
The present invention relates to a novel 3-aminobenzamide compound represented by the following formula which effectively inhibits vanilloid receptor subtype 1 (VR1) activity (wherein, for example, R1 is a C1-6 alkyl group which may be substituted, R2 is a hydrogen atom, a C1-6 alkyl group or a C1-6 alkoxy group which may be substituted, R3 is a hydrogen atom or a C1-6 alkyl group, R4 is a C1-6 alkyl group, a C1-6 alkoxy group, or a halo C1-6 alkyl group, m is an integer of 1 to 5 and P is a carbon or hetero ring) or a pharmaceutically acceptable salt thereof. The pharmaceutical composition comprising as active ingredients the 3-aminobenzamide compound or a pharmaceutically acceptable salt thereof is useful for treating diseases involved in VR1 activity such as pain, acute pain, chronic pain, neuropathic pain, rheumatoid arthritis pain, and neuralgia.
