Design, synthesis and pharmacological evaluation of 4-(3-chloro-4-(3-cyclopropylthioureido)-2-fluorophenoxy)-7-methoxyquinoline-6-carboxamide (WXFL-152): a novel triple angiokinase inhibitor for cancer therapy.
第一作者:
Yuqin,Yao
第一单位:
State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China School of Public Health and West China Fourth Hospital, Sichuan University, Chengdu 610041, China.;Guangdong Zhongsheng Pharmaceutical Co., Ltd., Dongguan 523325, China.;West China School of Public Health and West China Fourth Hospital, Healthy Food Evaluation Research Center, Sichuan University, Chengdu 610041, China.
作者:
关键词
ATCC, American Type Culture CollectionAUC, area under the plasma concentration–time curveAnti-angiogenesis therapyCE, collision energyCL, systemic clearanceCmax, maximum plasma concentrationDrug synthesisEC, vascular endothelial cellECM, endothelial cell mediumERKs, extracellular signal-regulated kinasesFGF, fibroblast growth factorFGFRs, fibroblast growth factor receptorsHBVPs, human brain vascular pericytesHUVECs, human umbilical vein endothelial cellsIC50, half maximal inhibitory concentrationIHC, immunohistochemistryLC–MS, liquid chromatography mass spectrometryLLOQ, lower limit of quantificationMRM, multiple reaction monitoringMsOH, methane sulfonic acidMulti-angiokinase inhibitorNMR, nuclear magnetic resonancePD, pharmacodynamicsPDB, protein data bankPDGF, platelet-derived growth factorPDGFRs, platelet-derived growth factor receptorsPDX, patient-derived tumor xenograftPK, pharmacokineticsPM, pericyte mediumPharmacokineticQC, quality controlRE, values and relative errorRSD, relative standard deviationRTKs, receptor tyrosine kinasesTGI, tumor growth inhibition rateTLC, thin-layer chromatographyTmax, time the maximum concentration occurredTumorULOQ, up limit of quantitationVEGF, vascular endothelial growth factorVEGFRs, vascular endothelial growth factor receptorsVdss, volume of distribution at steady statei.v., intravenous injectionp.o., per os
DOI
10.1016/j.apsb.2020.04.002
PMID
32963943
发布时间
2024-03-29
- 浏览3
Acta pharmaceutica Sinica. B
2020年10卷8期
1453-1475页
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