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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£©£º752-764 Çë°ïæ²éѯ¸ÃÎÄÊÇ·ñÒѱ»SCIÊÕ¼£¬Ð»Ð»£¡ |
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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 ×÷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¿·½Ïò lant Sciences; Chemistry; Pharmacology & PharmacyWeb of Science Àà±ð lant Sciences; Chemistry, Applied; Chemistry, Medicinal; Pharmacology & PharmacyÎÄÏ×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® |
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