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Development of o-aminobenzamide salt derivatives for improving water solubility and anti-undifferentiated gastric cancer

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成果类型:
期刊论文
作者:
Li, Shuang;He, Yanli;Li, Xuelin;Xiong, Yongxia;Peng, Yan;...
通讯作者:
Jiang, Weifan;Wang, Z;Lu, XZ
作者机构:
[Peng, Yan; Li, Shuang; Wang, Zhen; Zhuo, Linsheng; Jiang, Weifan; Xiong, Yongxia; Li, Xuelin] Univ South China, Hengyang Med Sch, Sch Pharmaceut Sci, Hengyang, Hunan, Peoples R China.
[He, Yanli] Univ South China, Affiliated Nanhua Hosp, Hengyang Med Sch, Dept Pain Rehabil, Hengyang, Hunan, Peoples R China.
[Lu, Xianzhou] Univ South China, Affiliated Nanhua Hosp, Hengyang Med Sch, Dept Hepatobiliary Surg, Hengyang, Hunan, Peoples R China.
[Wang, Chengkun] Univ South China, Canc Res Inst, Hengyang Med Sch, Hunan Prov Key Lab Tumor Cellular & Mol Pathol, Hengyang, Peoples R China.
[Wang, Zhen; Zhuo, Linsheng] Univ South China, Hengyang Med Sch, Postdoctoral Stn Basic Med, Hengyang, Hunan, Peoples R China.
通讯机构:
[Jiang, WF; Wang, Z ; Lu, XZ ]
Univ South China, Hengyang Med Sch, Sch Pharmaceut Sci, Hengyang, Hunan, Peoples R China.
Univ South China, Affiliated Nanhua Hosp, Hengyang Med Sch, Dept Hepatobiliary Surg, Hengyang, Hunan, Peoples R China.
Univ South China, Hengyang Med Sch, Postdoctoral Stn Basic Med, Hengyang, Hunan, Peoples R China.
语种:
英文
关键词:
antitumor;o-aminobenzamide derivate;salt formation;undifferentiated gastric cancer;water solubility
期刊:
Frontiers in Pharmacology
ISSN:
1663-9812
年:
2023
卷:
14
页码:
1118397
基金类别:
This research was supported by Gansu Province Science Foundation for Distinguished Young Scholars (No. 20JR5RA304), National Natural Science Foundation of China (No. 22107034), China Postdoctoral Science Foundation (2022M721544), Hunan Provincial Natural Science Foundation of China (No. 2022JJ40356, 2023JJ40571, 2023JJ30527), Key Research Project of Science and Technology Department of Hunan Province (No. 2020SKC2009) and Major Research Fund of Hunan Provincial Health and Family Planning Commission (No. A2017012).
机构署名:
本校为第一且通讯机构
院系归属:
医学院
摘要:
Background: Gastric cancer is one of the cancers with wide incidence, difficult treatment and high mortality in the world, especially in Asia and Africa. In our previous work, a novel o-aminobenzamide analogue F8 was identified as an early preclinical candidate for treatment of undifferentiated gastric cancer (IC50 of 0.26μM for HGC-27). However, the poor water solubility of compound F8 prevents its further progress in preclinical studies. Aim: To improve the water solubility and drug-likeness of F8 via salt formation. Method: Different acids ...

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