Mayumi Yamaoka, Mitsuji Yamashita, Manabu Yamada, Michio Fujie, Keita Kiyofuji, Nobuhisa Ozaki, Kazuhide Asai, Taishi Niimi, Takuya Suyama, Junko Yamashita, Akiho Sawada, Reiko Makita, Masaki Sugiyama, Mitsuo Toda, Satoki Nakamura, Kazunori Ohnishi
December 27, 2011
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.