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Starting materials of phosphasugars, 1-phenyl-2-phospholene 1-oxides, were prepared from dienes and phenylphosphonous dichloride (dichlorophenylphosphine). Several substituted novel phosphasugars (3- or 4-halo-substituted)-1-phenyl-2-phospholene 1-oxides as well as 1-phenyl-2-phospholane 1-oxides were prepared from 2-phospholenes. The synthesized compounds were evaluated for their antitumor activities against the leukemia cell lines (U937 and K562) by in vitro 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. 2,3,4-Tribromo-3-methyl-1-phenylphospholane 1-oxide showed superior antitumor activity against U937 and K562 cell lines in a comparative evaluation with Glivec. The analysis by flow cytometry implied that 2,3-dibromo-3-methyl-1-phenylphospholane 1-oxide induced apoptosis to leukemia cell lines.

Novel Sugar Dendritic Gd(III)-DTPA complexes for MRI Contrast Agents (CAs) were prepared and evaluated by in vitro and in vivo methods. The sugar dendritic MRI contrast agents had a good blood vessel pool character and drew blood vessels and liver cancers remarkably clearer and longer time enough than the clinically being used Gd(III)-DTPA complex (Magnevist). Phospha sugar derivatives or phosphorus heterocyclic derivatives provided by functional groups such as epoxide, bromide, etc., were prepared and evaluated by the MTT in vitro method. These phospha sugar derivatives showed excellent anti-proliferative effects of leukemia cell lines, e.g., K562 and U937, as well as solid cancer cells in fashions of (i) higher activity, (ii) wider spectra, and (iii) higher selectivity and specificity than Imatinib mesylate (Gleevec), which is one of the most frequently used chemotherapeutical molecular targeting anti-tumour agent.