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【答案】应助回帖
★ ★ ★ ★ ★
感谢参与，应助指数 +1
龙凤呈祥: 金币+5, ★★★★★最佳答案, 非常感谢！ 2016-08-28 22:03:27
lazy锦溪: LS-EPI+1 2016-08-28 22:52:56
https://apps.webofknowledge.com/ ... age=1&doc=1
New C-19-modified geldanamycin derivatives: synthesis, antitumor activities, and physical properties study
作者:Liu, YF (Liu, Yu-Feng)[ 1,2,3 ] ; Zhong, JJ (Zhong, Jing-Jing)[ 1,2 ] ; Lin, L (Lin, Ling)[ 1,2 ] ; Liu, JJ (Liu, Juan-Juan)[ 1,2 ] ; Wang, YG (Wang, Yi-Guang)[ 1,2 ] ; He, WQ (He, Wei-Qing)[ 1,2 ] ; Yang, ZY (Yang, Zhao-Yong)[ 1,2 ]
JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH
卷: 18
期: 8
页: 752-764
DOI: 10.1080/10286020.2016.1160896
出版年: 2016
查看期刊信息
JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH
出版商 TAYLOR & FRANCIS LTD, 2-4 PARK SQUARE, MILTON PARK, ABINGDON OR14 4RN, OXON, ENGLAND
ISSN: 1028-6020
eISSN: 1477-2213
研究领域 Plant Sciences
Chemistry
Pharmacology & Pharmacy
摘要
Thiazinogeldanamycin (2) was identified from Streptomyces hygroscopicus 17997 at the late stage of the fermentation. The pH was firstly proposed as an important factor in the biosynthesis of it. It was verified that 2 was produced by direct chemical reactions between geldanamycin (1, GDM) and cysteine or aminoethanethiol hydrochloride at pH>7 in vitro. The proposed synthesis pathway for compound 2 was also discussed. Eleven new C-19-modified GDM derivatives, including five stable hydroquinone form derivatives, were synthesized, most of which exhibited desirable properties such as lower cytotoxicity, increased water solubility, and potent antitumor activity. Especially, compounds 5 and 8 showed antitumor activities against HepG2 cell with IC50 values of 2.97-6.61M, lower cytotoxicity and at least 15-fold higher water solubility compared with 1 in pH 7.0 phosphate buffer.
关键词
作者关键词:C-19-modified geldanamycin derivatives; synthesis; antitumor activity; stability; water solubility
KeyWords Plus:STREPTOMYCES-HYGROSCOPICUS 17997; SHOCK-PROTEIN 90; BIOLOGICAL EVALUATION; IN-VITRO; HSP90; INHIBITORS; IDENTIFICATION; ANALOGS
作者信息
通讯作者地址: He, WQ; Yang, ZY (通讯作者) Chinese Acad Med Sci, Inst Med Biotechnol, Beijing 100050, Peoples R China.
增强组织信息的名称
Chinese Academy of Medical Sciences - Peking Union Medical College
Institute of Medicinal Biotechnology - CAMS
通讯作者地址: He, WQ; Yang, ZY (通讯作者) Peking Union Med Coll, Beijing 100050, Peoples R China.
增强组织信息的名称
Chinese Academy of Medical Sciences - Peking Union Medical College
地址: [ 1 ] Chinese Acad Med Sci, Inst Med Biotechnol, Beijing 100050, Peoples R China
增强组织信息的名称
Chinese Academy of Medical Sciences - Peking Union Medical College
Institute of Medicinal Biotechnology - CAMS
[ 2 ] Peking Union Med Coll, Beijing 100050, Peoples R China
增强组织信息的名称
Chinese Academy of Medical Sciences - Peking Union Medical College
[ 3 ] Jining Med Univ, Dept Pharm, Jining 272067, Peoples R China
增强组织信息的名称
Jining Medical University
电子邮件地址:Heweiqing@imb.pumc.edu.cn; zhaoyongy@163.com
基金资助致谢
基金资助机构 授权号
Natural Science Foundation of China 81172965
81172972
81261120417
PUMC Youth Foundation 3332015166
查看基金资助信息关闭基金资助信息
This work was supported by the financial support from Natural Science Foundation of China [grant number 81172965], [grant number 81172972], [grant number 81261120417]; PUMC Youth Foundation [grant number 3332015166].
出版商
TAYLOR & FRANCIS LTD, 2-4 PARK SQUARE, MILTON PARK, ABINGDON OR14 4RN, OXON, ENGLAND
类别 / 分类
研究方向 lant Sciences; Chemistry; Pharmacology & Pharmacy
Web of Science 类别lant Sciences; Chemistry, Applied; Chemistry, Medicinal; Pharmacology & Pharmacy
文献信息
文献类型:Article
语种:English
入藏号: WOS:000379739300006
PubMed ID: 26988280
ISSN: 1028-6020
eISSN: 1477-2213
其他信息
IDS 号: DR2MT
Web of Science 核心合集中的 "引用的参考文献": 21
Web of Science 核心合集中的 "被引频次": 0
JCR® 类别 JCR 分区
CHEMISTRY, APPLIED Q3
CHEMISTRY, MEDICINAL Q4
PHARMACOLOGY & PHARMACY Q4
PLANT SCIENCES Q3
数据来自第 2015 版 Journal Citation Reports® |
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