The preparation of bi-functional organophosphine oxides as potential antitumor agents

Kim Hung Lam*, Chung Hin CHUI, Roberto Gambari, Raymond Siu Ming Wong, Gregory Yin Ming Cheng, Fung Yi Lau, Paul Bo San Lai, See Wai Tong, Kit Wah Chan, Wai Yeung WONG, Albert Sun Chi Chan, Johnny Cheuk On Tang

*Corresponding author for this work

Research output: Contribution to journalJournal articlepeer-review

16 Citations (Scopus)


Following our previously reported pyridinyl phosphine oxides as antitumor agents, we targeted the commercially available C2-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.

Original languageEnglish
Pages (from-to)5527-5530
Number of pages4
JournalEuropean Journal of Medicinal Chemistry
Issue number11
Publication statusPublished - Nov 2010

Scopus Subject Areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

User-Defined Keywords

  • Antitumor activity
  • Bi-functional organophosphine oxides
  • Hepatocellular carcinoma


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