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Stereoselective synthesis of 3,3-diarylacrylonitriles as tubulin polymerization inhibitors
被引:19
|作者:
Fang, Zhenglai
[1
,2
]
Song, Yunlong
[1
,2
]
Sarkar, Taradas
[3
]
Hamel, Ernest
[3
]
Fogler, William E.
[4
]
Agoston, Gregory E.
[4
]
Fanwick, Phillip E.
[5
]
Cushman, Mark
[1
,2
]
机构:
[1] Purdue Univ, Sch Pharm & Pharmaceut Sci, Dept Med Chem & Mol Pharmacol, W Lafayette, IN 47907 USA
[2] Purdue Univ, Purdue Canc Ctr, W Lafayette, IN 47907 USA
[3] Natl Inst Hlth, Natl Canc Inst, Div Canc Treatment & Diag, Dev Therapeut Program,Toxicol & Pharmacol Branch, Frederick, MD 21702 USA
[4] EntreMed Inc, Rockville, MD 20850 USA
[5] Purdue Univ, Dept Chem, W Lafayette, IN 47907 USA
来源:
关键词:
D O I:
10.1021/jo800428b
中图分类号:
O62 [有机化学];
学科分类号:
070303 ;
081704 ;
摘要:
A series of 3,3-diarylacrylonitriles were synthesized stercoselectively as tubulin polymerization inhibitors for potential use in cancer chemotherapy. This synthetic route features stannylcupration and palladium-catalyzed Stille cross-coupling chemistry, allowing both E and Z isomers of 3,3-diarylacrylonitriles to be prepared in a very short sequence of reactions.
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页码:4241 / 4244
页数:4
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