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Research and development of phospha sugar anti-cancer agents with anti-leukemic activity

DOI: 10.1515/HC.2010.16.2-3.89

Source and publish data:

Heterocyclic Communications p. 89 - 97 (2010)

Update date:2022-08-11

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Authors:

Yamashita, JunkoYamashita, Junko

Suyamab, TakuyaSuyamab, Takuya

Asai, KazuhideAsai, Kazuhide

Yamada, ManabuYamada, Manabu

Niimi, TaishiNiimi, Taishi

Fujie, MichioFujie, Michio

Nakamura, SatokiNakamura, Satoki

Ohnishi, KazunoriOhnishi, Kazunori

Yamashita, MitsujiYamashita, Mitsuji

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Article abstract of DOI:10.1515/HC.2010.16.2-3.89

We have synthesized three deoxybromophospha sugar analogues, 4-bromo-3-methyl-l-phenyl-2-phospholene 1-oxide (MBMPP (2)), 2,3-dibromo-3-methyl-l-phenylphospholane 1-oxide (DBMPP (3)), and 2,3,4-tribromo-3-methyl-1-phenylphospholane 1-oxide (TBMPP (4)), by the reaction of 3-methyl-l-phenyl-2-phospholene 1-oxide (lb) and/or 2 with bromine, and investigated their potentials as anti-leukemic agents against human leukemia cell lines of K562 and U937. Cells' growth inhibition was determined by using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) in vitro assay. All agents showed inhibitory effects on leukemia cell proliferation, indicating that inhibition appeared to be dependent on number of bromine substituent in the heterocyclic structure. Further, the phospha sugar derivatives did not show any inhibitory effects on normal cell proliferation. These agents may facilitate the development of new strategies in molecular targeting anti-leukemic therapy.

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Full text of DOI:10.1515/HC.2010.16.2-3.89

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Brought to you by | University of Arizona  
Authenticated  
Download Date | 10/13/15 11:58 PM  
Brought to you by | University of Arizona  
Authenticated  
Download Date | 10/13/15 11:58 PM  
Brought to you by | University of Arizona  
Authenticated  
Download Date | 10/13/15 11:58 PM  
Brought to you by | University of Arizona  
Authenticated  
Download Date | 10/13/15 11:58 PM  
Brought to you by | University of Arizona  
Authenticated  
Download Date | 10/13/15 11:58 PM  
Brought to you by | University of Arizona  
Authenticated  
Download Date | 10/13/15 11:58 PM  
Brought to you by | University of Arizona  
Authenticated  
Download Date | 10/13/15 11:58 PM  
Brought to you by | University of Arizona  
Authenticated  
Download Date | 10/13/15 11:58 PM  
Brought to you by | University of Arizona  
Authenticated  
Download Date | 10/13/15 11:58 PM  

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Product name:2,3,4-tribromo-3-methyl-1-phenylphospholane 1-oxide

Cas No:1050329-12-8

1050329-12-8

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