The Preparation and Anticancer Activity of Some Phosphorus Heterocycles

Abstract

Methods for the preparation of some phosphorus heterocycles are reviewed, together with a preliminary report of their activity in vitro against the NCI 60-cell line panel of human tumour cells. The most active compound, a dimer of 3-methyl-1-(2,4,6-triisopropylphenyl)phosphole oxide, showed GI₅₀ values in the micromolar region against leukaemia cell lines RPMI-8226 and SR, non-small cell lung cancer (NCI-H460), colon cancer (COLO 205), and melanoma (SK-Mel-5 and UACC-62).

Keywords:

• Anticancer
• dihydrophosphinine
• NCI
• organophosphorus
• phosphanorbornene
• phosphole oxide
• phosphorus heterocycle
• tetrahydrophosphinine

Acknowledgments

We thank the National Cancer Institute ¹¹ for anticancer screening and for the biological data reported in this paper. This project was also supported by the Hungarian Scientific Research Fund (OTKA Grant No. T067679).

Notes

^aData from the DTP website (http://dtp.nci.nih.gov), where full information is given for compounds 3 (NSC 709166), 5 (NSC 709160), 8a (NSC 639390), 8b (NSC 644257), 8c (NSC 639391), 13a (NSC 644259), 13c (NSC 648099), 13d (NSC 648100), and 13e (NSC 624332).

^bMolar concentrations for 50% growth inhibition (GI₅₀), total growth inhibition (TGI), and 50% kill (LC₅₀).

^aNegative values indicate the level of kill. Positive values indicate growth inhibition by at least 50%.