The preparation of bi-functional organophosphine oxides as potential antitumor agents
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摘要Following our previously reported pyridinyl phosphine oxides as antitumor agents, we targeted the commercially available C-2-axial chiral organophosphine ligand catalysts, such as 2,2'-bis(diphenylphosphino)-1,1'-binaphthyl (BINAP) 1 and 2,2',6,6'-tetramethoxy-4,4'-bis(diphenylphosphino)-3,3'-bipyridine (P-Phos) 2 as a convenient source for producing organophosphine oxides as antitumor leads. Their corresponding chiral and racemic bi-phosphine oxides 3 and 4 can be obtained easily through a simple oxidation step with hydrogen peroxide, and their antitumor activities towards human hepatocellular carcinoma Hep3B cell line were reported. We found out that compound 3 shows stronger antitumor activity than that of 4, where axial chirality cannot improve their activity. Further athymic nude mice Hep3B xenograft model demonstrates the attractive in vivo antitumor potential of 3. (C) 2010 Elsevier Masson SAS. All rights reserved.
著者Lam KH, Chui CH, Gambari R, Wong RSM, Cheng GYM, Lau FY, Lai PBS, Tong SW, Chan KW, Wong WY, Chan ASC, Tang JCO
期刊名稱European Journal of Medicinal Chemistry
出版年份2010
月份11
日期1
卷號45
期次11
出版社Elsevier
頁次5527 - 5530
國際標準期刊號0223-5234
電子國際標準期刊號1768-3254
語言英式英語
關鍵詞Antitumor activity; Bi-functional organophosphine oxides; Hepatocellular carcinoma
Web of Science 學科類別Chemistry, Medicinal; CHEMISTRY, MEDICINAL; Pharmacology & Pharmacy

上次更新時間 2020-24-11 於 23:59