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ÌâÄ¿£ºSynthesis and bioactivity of new Finasteride conjugate.
×÷ÕߣºShuang, Zhao   Jiazhen, Wu   Lijuan, Yang   Zhuo, Li   Dahai, Yu   Jinfeng, Li   Jing, Yu   Yongtao, Liang   En-Si, Wang   Xuexun, Fang
·¢±íÈÕÆÚ£º2011 £¬ÆÚ¾í£¬Ò³Â룺21(11):3439-42.
Á´½Ó£ºhttp://www.sciencedirect.com/sci ... i/S0960894X11004318
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±êÌâ: Synthesis and bioactivity of new Finasteride conjugate  
×÷Õß: Zhao, S (Zhao Shuang); Wu, JZ (Wu Jiazhen); Yang, LJ (Yang Lijuan); Li, Z (Li Zhuo); Yu, DH (Yu Dahai); Li, JF (Li Jinfeng); Yu, J (Yu Jing); Liang, YT (Liang Yongtao); Wang, ES (Wang En-si); Fang, XX (Fang Xuexun)
À´Ô´³ö°æÎï: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS  ¾í: 21  ÆÚ: 11  Ò³: 3439-3442  DOI: 10.1016/j.bmcl.2011.03.102  ³ö°æÄê: JUN 1 2011   
ÔÚ Web of Science Öеı»ÒýƵ´Î: 0  
±»ÒýƵ´ÎºÏ¼Æ: 0  
ÒýÓõIJο¼ÎÄÏ×Êý: 30  
ÕªÒª: Finasteride is a synthetic 4-azasteroid compound that acts by inhibiting type II 5 alpha-reductase, the enzyme that converts the androgen testosterone to 5 alpha-dihydrotestosterone. It was approved by the US FDA for the treatment of benign prostatic hyperplasia and male pattern baldness. Here the acylation product of Finasteride C-18 amide N-polimod was synthesized by employing acylation reaction with polimod amide as a pivotal intermediate. The structure of the key intermediate and target molecule was confirmed by infrared spectrum, (1)H NMR and (13)C NMR spectra and mass spectrum, and the inhibition of the steroid 5 alpha-reductase and the rats' benign prostatic hyperplasia by the new Finasteride conjugate and Finasteride was also determined. The inhibition of the Finasteride conjugate on 5 alpha-reductase was stronger than that of Finasteride. Prostate hyperplasia of rats was reduced by Finasteride conjugate treatment similar to the Finasteride treatment. However, the Finasteride conjugate treated animals showed better viable condition than the Finasteride treated ones, suggesting the new compound may have improved toxicity profile than Finasteride. (C) 2011 Elsevier Ltd. All rights reserved.
Èë²ØºÅ: WOS:000290708300053  
ÓïÖÖ: English
ÎÄÏ×ÀàÐÍ: Article
×÷Õ߹ؼü´Ê: Synthesis; Finasteride; Conjugates; 5 alpha-Reductase; Polimod
KeyWords Plus: BENIGN PROSTATIC HYPERPLASIA; STEROID 5-ALPHA-REDUCTASE; INHIBITORS; MEN
µØÖ·: [Zhao Shuang; Li Zhuo; Liang Yongtao; Wang En-si] Jilin Univ, Coll Life Sci, Changchun 130021, Peoples R China.
[Wu Jiazhen; Yu Dahai; Fang Xuexun] Jilin Univ, Key Lab Mol Enzymol & Enzyme Engn, Minist Educ, Changchun 130012, Peoples R China.
[Yang Lijuan; Yu Jing; Wang En-si] Jilin Univ, Coll Pharm, Changchun 130021, Peoples R China.
[Wu Jiazhen] Chinese Acad Sci, State Key Lab Electroanalyt Chem, Changchun Inst Appl Chem, Changchun 130022, Peoples R China.
[Li Jinfeng] Sun Yat Sen Univ, Sun Yat Sen Mem Hosp, Guangzhou 510120, Guangdong, Peoples R China.  
ͨѶ×÷ÕßµØÖ·: Wang, ES (ͨѶ×÷Õß),Jilin Univ, Coll Life Sci, Changchun 130021, Peoples R China.
µç×ÓÓʼþµØÖ·: dahaiyu.lipase@yahoo.com.cn
³ö°æÉÌ: PERGAMON-ELSEVIER SCIENCE LTD  
³ö°æÉ̵ØÖ·: THE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLAND  
Web of Science Àà±ð: Chemistry, Medicinal; Chemistry, Organic
Ñо¿·½Ïò: Pharmacology & Pharmacy; Chemistry
IDS ºÅ: 765LR  
ISSN: 0960-894X  
29 ×Ö·ûµÄÀ´Ô´³ö°æÎïÃû³ÆËõд: BIOORG MED CHEM LETT  
ISO À´Ô´³ö°æÎïËõд: Bioorg. Med. Chem. Lett.  
À´Ô´³ö°æÎïÒ³Âë¼ÆÊý: 4
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