Synthesis and anticancer activity of new class of bisphosphonates/phosphanamidates.

Abstract Novel bis-heterocyclic bisphosphonates/phosphonamidates were synthesized utilizing the Pudovick reaction. The employment of Nb 2 O 5 as catalyst was found to increase the yields and purity of the bisbenzoxazaphosphine derivatives ( 13a – h ). Their anticancer activity studies in vitro , on three human tumor cell lines NCI-H460 (lung large cell), MCF-7 (breast adenocarcinoma), and SF-268 (central nervous system glioblastoma), showed that bis-[3-(3-chloro-4-fluorophenyl)-2-oxo-3,4-dihydro-2H-2λ 5 -benzo[ e ][1,3,2]oxazaphosphinin-2-yl]arylmethanes ( 13a – h ) and [(4-chlorophenyl)-(hydroxyamidophosphinoyl)-methyl]phosphonic acid ( 14 ) exhibited significant anticancer activity.