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The synthesis and antitumor activity evaluation of new branched phospha sugars, especially deoxybromophospha sugar derivatives or bromophospholanes of 2,3-dibromo-3-methyl-1-phenylphospholane 1-oxide (DBMPP: 3) and 2,3,4-tribromo-3-methyl-1- phenylphospholane 1-oxide (TBMPP: 4), against various types of leukemia cell lines as well as the results of the mechanistic studies for characterizing and developing the novel multiple type molecular targeted antitumor agents are reported in this paper. DBMPP and TBMPP were prepared from 1-phenyl-3-methyl-2-phospholene 1-oxide (1). The isomer mixture of phospha sugars prepared were evaluated as novel antitumor agents by MTT in vitro method. DBMPP and TBMPP were characterized by flow cytometry and Western blot analysis and were revealed to be potential antitumor agents against leukemia cell lines of K562 (one type of leukemia cell lines of CML) and U937 (one type of leukemia cell lines of AML) as well as against the various types of leukemia cell lines and al...

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.

浜松市内の環境水中に含まれる腐植物質及びその他の蛍光物質を三次元蛍光スペクトルを測定して検討した。励起波長345nm, 蛍光波長430nm付近の蛍光ピークの蛍光強度と250nmの吸光度との間には相関性が認められた。種々の孔径のろ紙及びメンブランフィルターによる環境水のろ過について検討した結果, 蛍光物質によってろ過処理効果が異なるので, 環境水をろ過処理する場合, 三次元蛍光スペクトルを比較して適当なろ紙又はメンブランフィルターを選択することが必要である。8種類の固相抽出用カートリッジを用いて固相抽出処理を検討した。固相抽出処理では蛍光物質の種類, 溶存状態に関係なく蛍光物質を除去でき, AC2カートリッジを用いると, ほぼ100%蛍光物質を除去できた。

Hiroko Hasegawa, Mitsuji Yamashita,* Reiko Makita, Mayumi Yamaoka, Michio Fujie, Satoki Nakamura, Tatsuo Oshikawa, Junko Yamashita, Manabu Yamada, Mitsuru Kondo, Kazutaka Hirakawa, Mitsuo Toda, Yasuo Takehara, Kazunori Ohnishi, Haruhiko Sugimura, Sophie Laurent, and Robert N. Muller 1 Graduate School of Science and Technology, Shizuoka University, Hamamatsu 432-8561, Japan 2 Faculty of Medicine, Hamamatsu University School of Medicine, Hamamatsu 431-3192, Japan 3 Department of Chemistry and Biochemistry, Numazu National College of Technology, Numazu 410-8501, Japan 4 Faculty of Medicine, University of Mons, Mons, Hainaut, Belgium