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Yufeng Liu, Jingjing Zhong, Ling Lin, Juanjuan Liu, Yiguang Wang, Weiqing He, Zhaoyong Yang*, New C-19 Modified Geldanamycin Derivatives: Synthesis, Antitumor Activities and Physical Properties Study. J. Asian Nat. Prod. Res., 2016，18（8）：752-764
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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
頁: 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

研究領(lǐng)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.

關(guān)鍵詞
作者關(guān)鍵詞: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
通訊作者地址: He, WQ; Yang, ZY (通訊作者) Chinese Acad Med Sci, Inst Med Biotechnol, Beijing 100050, Peoples R China.
  增強(qiáng)組織信息的名稱
Chinese Academy of Medical Sciences - Peking Union Medical College
Institute of Medicinal Biotechnology - CAMS
通訊作者地址: He, WQ; Yang, ZY (通訊作者) Peking Union Med Coll, Beijing 100050, Peoples R China.
  增強(qiáng)組織信息的名稱
Chinese Academy of Medical Sciences - Peking Union Medical College

地址:  [ 1 ] Chinese Acad Med Sci, Inst Med Biotechnol, Beijing 100050, Peoples R China
  增強(qiáng)組織信息的名稱
Chinese Academy of Medical Sciences - Peking Union Medical College
Institute of Medicinal Biotechnology - CAMS
[ 2 ] Peking Union Med Coll, Beijing 100050, Peoples R China
  增強(qiáng)組織信息的名稱
Chinese Academy of Medical Sciences - Peking Union Medical College
[ 3 ] Jining Med Univ, Dept Pharm, Jining 272067, Peoples R China
  增強(qiáng)組織信息的名稱
Jining Medical University

電子郵件地址:Heweiqing@imb.pumc.edu.cn; zhaoyongy@163.com

基金資助致謝
基金資助機(jī)構(gòu) 授權(quán)號
Natural Science Foundation of China  81172965
81172972
81261120417
PUMC Youth Foundation  3332015166
查看基金資助信息關(guān)閉基金資助信息

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

類別 / 分類
研究方向

lant Sciences; Chemistry; Pharmacology & Pharmacy

Web of Science 類別

lant Sciences; Chemistry, Applied; Chemistry, Medicinal; Pharmacology & Pharmacy

文獻(xiàn)信息
文獻(xiàn)類型:Article

語種:English

入藏號: WOS:000379739300006

PubMed ID: 26988280

ISSN: 1028-6020

eISSN: 1477-2213

其他信息
IDS 號: DR2MT

Web of Science 核心合集中的 "引用的參考文獻(xiàn)": 21

Web of Science 核心合集中的 "被引頻次": 0

JCR® 類別 JCR 分區(qū)
CHEMISTRY, APPLIED  Q3
CHEMISTRY, MEDICINAL  Q4
PHARMACOLOGY & PHARMACY  Q4
PLANT SCIENCES  Q3

數(shù)據(jù)來自第 2015 版 Journal Citation Reports®

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