²é¿´: 148  |  »Ø¸´: 1
±¾Ìû²úÉú 1 ¸ö £¬µã»÷ÕâÀï½øÐв鿴

Áú·ï³ÊÏé

Ìú¸Ëľ³æ (ÖøÃûдÊÖ)

[ÇóÖú] SCIÊÕ¼²éѯ

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£©£º752-764
Çë°ïæ²éѯ¸ÃÎÄÊÇ·ñÒѱ»SCIÊÕ¼£¬Ð»Ð»£¡

» ²ÂÄãϲ»¶

ÒÑÔÄ   »Ø¸´´ËÂ¥   ¹Ø×¢TA ¸øTA·¢ÏûÏ¢ ËÍTAºì»¨ TAµÄ»ØÌû

baiyuefei

°æÖ÷ (ÎÄѧ̩¶·)

·çÑ©

ÓÅÐã°æÖ÷ÓÅÐã°æÖ÷ÓÅÐã°æÖ÷ÎÄÏ׽ܳö¹±Ï×ÓÅÐã°æÖ÷ÓÅÐã°æÖ÷ÓÅÐã°æÖ÷ÎÄÏ׽ܳö¹±Ï×ÓÅÐã°æÖ÷ÓÅÐã°æÖ÷ÓÅÐã°æÖ÷ÓÅÐã°æÖ÷ÎÄÏ׽ܳö¹±Ï×ÓÅÐã°æÖ÷ÓÅÐã°æÖ÷ÓÅÐã°æÖ÷ÓÅÐã°æÖ÷ÓÅÐã°æÖ÷ÓÅÐã°æÖ÷

¡¾´ð°¸¡¿Ó¦Öú»ØÌû

¡ï ¡ï ¡ï ¡ï ¡ï
¸Ðл²ÎÓ룬ӦÖúÖ¸Êý +1
Áú·ï³ÊÏé: ½ð±Ò+5, ¡ï¡ï¡ï¡ï¡ï×î¼Ñ´ð°¸, ·Ç³£¸Ðл£¡ 2016-08-28 22:03:27
lazy½õϪ: 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
×÷Õß: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


¾í: 18
ÆÚ: 8
Ò³: 752-764
DOI: 10.1080/10286020.2016.1160896

³ö°æÄê: 2016

²é¿´ÆÚ¿¯ÐÅÏ¢

JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH  

³ö°æÉÌ TAYLOR & FRANCIS LTD, 2-4 PARK SQUARE, MILTON PARK, ABINGDON OR14 4RN, OXON, ENGLAND

ISSN: 1028-6020
eISSN: 1477-2213

Ñо¿ÁìÓò Plant Sciences
Chemistry
Pharmacology & Pharmacy



ÕªÒª
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.

¹Ø¼ü´Ê
×÷Õ߹ؼü´Ê: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

×÷ÕßÐÅÏ¢
ͨѶ×÷ÕßµØÖ·: He, WQ; Yang, ZY (ͨѶ×÷Õß) Chinese Acad Med Sci, Inst Med Biotechnol, Beijing 100050, Peoples R China.
  ÔöÇ¿×éÖ¯ÐÅÏ¢µÄÃû³Æ
    Chinese Academy of Medical Sciences - Peking Union Medical College
    Institute of Medicinal Biotechnology - CAMS  
ͨѶ×÷ÕßµØÖ·: He, WQ; Yang, ZY (ͨѶ×÷Õß) Peking Union Med Coll, Beijing 100050, Peoples R China.
  ÔöÇ¿×éÖ¯ÐÅÏ¢µÄÃû³Æ
    Chinese Academy of Medical Sciences - Peking Union Medical College  


µØÖ·:  [ 1 ] Chinese Acad Med Sci, Inst Med Biotechnol, Beijing 100050, Peoples R China
  ÔöÇ¿×éÖ¯ÐÅÏ¢µÄÃû³Æ
    Chinese Academy of Medical Sciences - Peking Union Medical College
    Institute of Medicinal Biotechnology - CAMS  
[ 2 ] Peking Union Med Coll, Beijing 100050, Peoples R China
  ÔöÇ¿×éÖ¯ÐÅÏ¢µÄÃû³Æ
    Chinese Academy of Medical Sciences - Peking Union Medical College  
[ 3 ] Jining Med Univ, Dept Pharm, Jining 272067, Peoples R China
  ÔöÇ¿×éÖ¯ÐÅÏ¢µÄÃû³Æ
    Jining Medical University  


µç×ÓÓʼþµØÖ·:Heweiqing@imb.pumc.edu.cn; zhaoyongy@163.com

»ù½ð×ÊÖúÖÂл
»ù½ð×ÊÖú»ú¹¹ ÊÚȨºÅ
Natural Science Foundation of China  81172965
81172972
81261120417  
PUMC Youth Foundation  3332015166  
²é¿´»ù½ð×ÊÖúÐÅÏ¢¹Ø±Õ»ù½ð×ÊÖúÐÅÏ¢   

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].

³ö°æÉÌ
TAYLOR & FRANCIS LTD, 2-4 PARK SQUARE, MILTON PARK, ABINGDON OR14 4RN, OXON, ENGLAND

Àà±ð / ·ÖÀà
Ñо¿·½Ïòlant Sciences; Chemistry; Pharmacology & Pharmacy

Web of Science Àà±ðlant Sciences; Chemistry, Applied; Chemistry, Medicinal; Pharmacology & Pharmacy

ÎÄÏ×ÐÅÏ¢
ÎÄÏ×ÀàÐÍ:Article

ÓïÖÖ:English

Èë²ØºÅ: WOS:000379739300006

PubMed ID: 26988280

ISSN: 1028-6020

eISSN: 1477-2213

ÆäËûÐÅÏ¢
IDS ºÅ: DR2MT

Web of Science ºËÐĺϼ¯ÖÐµÄ "ÒýÓõIJο¼ÎÄÏ×": 21

Web of Science ºËÐĺϼ¯ÖÐµÄ "±»ÒýƵ´Î": 0

JCR® Àà±ð JCR ·ÖÇø
CHEMISTRY, APPLIED  Q3
CHEMISTRY, MEDICINAL  Q4
PHARMACOLOGY & PHARMACY  Q4
PLANT SCIENCES  Q3


Êý¾ÝÀ´×ÔµÚ 2015 °æ Journal Citation Reports®
2Â¥2016-08-28 07:36:01
ÒÑÔÄ   »Ø¸´´ËÂ¥   ¹Ø×¢TA ¸øTA·¢ÏûÏ¢ ËÍTAºì»¨ TAµÄ»ØÌû
Ïà¹Ø°æ¿éÌø×ª ÎÒÒª¶©ÔÄÂ¥Ö÷ Áú·ï³ÊÏé µÄÖ÷Ìâ¸üÐÂ
×î¾ßÈËÆøÈÈÌûÍÆ¼ö [²é¿´È«²¿] ×÷Õß »Ø/¿´ ×îºó·¢±í
[¿¼ÑÐ] 326Çóµ÷¼Á +5 ŵ±´¶û»¯Ñ§½±êéê 2026-03-15 8/400 2026-03-21 19:33 by ColorlessPI
[¿¼ÑÐ] Ò»Ö¾Ô¸¶«»ª´óѧ¿ØÖÆÑ§Ë¶320Çóµ÷¼Á +3 Grand777 2026-03-21 3/150 2026-03-21 19:23 by ¼òÖ®-
[¿¼ÑÐ] 0703»¯Ñ§µ÷¼Á +11 ÄÝÄÝninicgb 2026-03-15 15/750 2026-03-21 19:15 by ColorlessPI
[¿¼ÑÐ] ²ÄÁϹ¤³Ìר˶ 348·ÖÇóµ÷¼Á +3 ¶¬´Ç. 2026-03-17 5/250 2026-03-21 18:47 by ѧԱ8dgXkO
[¿¼ÑÐ] 277²ÄÁÏ¿ÆÑ§Ó빤³Ì080500Çóµ÷¼Á +6 ×ÔÓɼå±ý¹û×Ó 2026-03-16 6/300 2026-03-21 17:21 by ѧԱ8dgXkO
[¿¼ÑÐ] 22 350 ±¾¿Æ985Çóµ÷¼Á£¬ÇóÀϵÇÊÕÁô +3 ÀîéóÄÐ003 2026-03-20 3/150 2026-03-21 13:28 by ²«»÷518
[¿¼ÑÐ] 0856²ÄÁÏר˶353Çóµ÷¼Á +3 NIFFFfff 2026-03-20 3/150 2026-03-21 10:23 by luoyongfeng
[¿¼ÑÐ] Çóµ÷¼Á +6 Mqqqqqq 2026-03-19 6/300 2026-03-21 08:04 by JourneyLucky
[¿¼ÑÐ] 265Çóµ÷¼Á +3 Jack?k?y 2026-03-17 3/150 2026-03-21 03:17 by JourneyLucky
[¿¼ÑÐ] 265Çóµ÷¼Á +9 ÁºÁºÐ£Ð£ 2026-03-17 9/450 2026-03-21 02:17 by JourneyLucky
[¿¼ÑÐ] 308Çóµ÷¼Á +3 °¢½ã°¢½ã¼Ò°¡ 2026-03-18 3/150 2026-03-20 23:24 by JourneyLucky
[¿¼ÑÐ] 321Çóµ÷¼Á +9 ºÎÈó²É123 2026-03-18 11/550 2026-03-20 23:19 by JourneyLucky
[¿¼ÑÐ] Çóµ÷¼ÁÒ»Ö¾Ô¸ÄϾ©º½¿Õº½Ìì´óѧ289·Ö +3 @taotao 2026-03-19 3/150 2026-03-20 21:34 by JourneyLucky
[¿¼ÑÐ] AÇøÏß²ÄÁÏѧµ÷¼Á +5 ÖÜÖÜÎÞ¼« 2026-03-20 5/250 2026-03-20 21:33 by laoshidan
[¿¼ÑÐ] Çóµ÷¼Á +3 eation27 2026-03-20 3/150 2026-03-20 19:32 by JourneyLucky
[¿¼ÑÐ] ²ÄÁÏÓ뻯¹¤×¨Ë¶µ÷¼Á +7 heming3743 2026-03-16 7/350 2026-03-20 19:31 by zhukairuo
[¿¼ÑÐ] 0854£¬¼ÆËã»úÀàÕÐÊÕµ÷¼Á +3 ºúÀ±ÌÀ·ÅÌÇ 2026-03-15 6/300 2026-03-18 12:09 by Éϰ¶Éϰ¶¡­¡­..
[¿¼ÑÐ] 334Çóµ÷¼Á +3 Ö¾´æ¸ßÔ¶ÒâÔÚ»úÐ 2026-03-16 3/150 2026-03-18 08:34 by lm4875102
[¿¼ÑÐ] ²ÄÁÏר˶326Çóµ÷¼Á +6 Ä«ìÏæ¦Ý· 2026-03-15 7/350 2026-03-17 17:10 by ruiyingmiao
[¿¼ÑÐ] 290Çóµ÷¼Á +3 p asserby. 2026-03-15 4/200 2026-03-17 16:35 by wangkm
ÐÅÏ¢Ìáʾ
ÇëÌî´¦ÀíÒâ¼û