56053-55-5Relevant academic research and scientific papers
Discovery of a Pyrimidinedione Derivative as a Potent and Orally Bioavailable Axl Inhibitor
Zhang, Hefeng,Peng, Xia,Dai, Yang,Shao, Jingwei,Ji, Yinchun,Sun, Yiming,Liu, Bo,Cheng, Xu,Ai, Jing,Duan, Wenhu
, p. 3956 - 3975 (2021)
The receptor tyrosine kinase Axl plays important roles in promoting cancer progression, metastasis, and drug resistance and has been identified as a promising target for anticancer therapeutics. We used molecular modeling-assisted structural optimization starting with the low micromolar potency compound 9 to discover compound 13c, a highly potent and orally bioavailable Axl inhibitor. Selectivity profiling showed that 13c could inhibit the well-known oncogenic kinase Met with equal potency to its inhibition of Axl superfamily kinases. Compound 13c significantly inhibited cellular Axl and Met signaling, suppressed Axl- and Met-driven cell proliferation, and restrained Gas6/Axl-mediated cancer cell migration or invasion. Furthermore, 13c exhibited significant antitumor efficacy in Axl-driven and Met-driven tumor xenograft models, causing tumor stasis or regression at well-tolerated doses. All these favorable data make 13c a promising therapeutic candidate for cancer treatment.
QUINOLINE DERIVATIVE
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Paragraph 0179, (2017/11/17)
This compound represented by general formula (I) and having a quinoline skeleton has a strong Axl inhibitory activity. Consequently, this compound can be a therapeutic agent for Axl-related diseases, for example, cancers such as acute myeloid leukemia, chronic myeloid leukemia, melanoma, breast cancer, pancreatic cancer and glioma, kidney diseases, immune system diseases and cardiovascular diseases.
PYRIDONE DERIVATIVE HAVING AFFINITY FOR CANNABINOID 2-TYPE RECEPTOR
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Page/Page column 63-64, (2008/06/13)
It was found that the compound having a binding activity to the cannabinoid type 2 receptor represented by the formula (I): wherein R' is a group represented by the formula: -Y1-Y2-Y3Ra wherein Y1 is single bond or the like; Y2 is -C(=O)-NH- or the like; Y3 is optionally substituted aryl or the like; R2 is hydrogen or the like; R3 is alkyl or the like; R4 is alkyl or the like; R5 is optionally substituted alkyl or the like; or R3 and R4 taken together with the adjacent atom form cyclic group or the like.
11β-Alkyl-2-azaestratrienes and intermediates
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, (2008/06/13)
11β-Alkyl-2-azaestratrienes, displaying valuable pharmacological properties, e.g. anti-viral and hypolipemic, are manufactured by a total synthesis originating with dihydroresorcinol.
7-Aza-6-alkoxy-1-tetralones
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, (2008/06/13)
The preparation of 7-aza-6-alkoxy-1-tetralones which originates with dihydroresorcinol is disclosed herein. The subject compounds are useful intermediates in the synthesis of various compounds which possess valuable pharmacological properties.
