Document Type

Journal Article

Department/Unit

Department of Chemistry

Title

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

Language

English

Abstract

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. © 2010 Elsevier Masson SAS. All rights reserved.

Keywords

Antitumor activity, Bi-functional organophosphine oxides, Hepatocellular carcinoma

Publication Date

2010

Source Publication Title

European Journal of Medicinal Chemistry

Volume

45

Issue

11

Start Page

5527

End Page

5530

Publisher

Elsevier

DOI

10.1016/j.ejmech.2010.08.038

ISSN (print)

02235234

ISSN (electronic)

17683254

This document is currently not available here.

Share

COinS