The preparation of bi-functional organophosphine oxides as potential antitumor agents
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AbstractFollowing 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.
All Author(s) ListLam KH, Chui CH, Gambari R, Wong RSM, Cheng GYM, Lau FY, Lai PBS, Tong SW, Chan KW, Wong WY, Chan ASC, Tang JCO
Journal nameEuropean Journal of Medicinal Chemistry
Volume Number45
Issue Number11
Pages5527 - 5530
LanguagesEnglish-United Kingdom
KeywordsAntitumor activity; Bi-functional organophosphine oxides; Hepatocellular carcinoma
Web of Science Subject CategoriesChemistry, Medicinal; CHEMISTRY, MEDICINAL; Pharmacology & Pharmacy

Last updated on 2020-24-11 at 23:59