Preparation and characterization of novel 4-bromo-3,4-dimethyl-1-phenyl-2-phospholene 1-oxide and the analogous phosphorus heterocycles or phospha sugars
4-Bromo-3,4-dimethyl-1-phenyl-2-phospholene 1-oxide ( 3c) was first synthesized from 3,4-dimethyl-1-phenyl-2-phospholene 1-oxide ( 2c) by a bromo-radical substitution reaction occurred at C-4 position by NBS and AIBN. The novel phospha sugar analogue exerted high anti-proliferative effect on U937 ce...
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Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2010-10, Vol.20 (19), p.5943-5946 |
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Hauptverfasser: | , , , , , , , , , , |
Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | 4-Bromo-3,4-dimethyl-1-phenyl-2-phospholene 1-oxide (
3c) was first synthesized from 3,4-dimethyl-1-phenyl-2-phospholene 1-oxide (
2c) by a bromo-radical substitution reaction occurred at C-4 position by NBS and AIBN. The novel phospha sugar analogue exerted high anti-proliferative effect on U937 cells evaluated by MTT in vitro methods and was much more efficient than that of Gleevec®, which is known as a molecule targeting chemotherapeutical agent.
4-Bromo-3,4-dimethyl-1-phenyl-2-phospholene 1-oxide (
3c) was first synthesized from 3,4-dimethyl-1-phenyl-2-phospholene 1-oxide (
2c) by a bromo-radical substitution reaction occurred at C-4 position by
N-bromosuccinimide and 2,2′-azobisisobutyronitrile. The novel phospha sugar analogue
3c exerted high anti-proliferative effect on U937 cells evaluated by MTT in vitro methods and was much more efficient than that of Gleevec®, which is known as a molecule targeting chemotherapeutical agent. The substitution of 2-phospholenes at C-3 and C-4 position with methyl groups as well as 4-bromo substituent suggests a good anti-proliferative effect. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2010.01.061 |