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| Total synthesis and anticancer activity studies of the stereoisomers of asperphenamate and patriscabratine |
| Lei Yuana, Jin Hui Wangb, Tie Min Suna |
a School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China;
b School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, China |
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Abstract All stereoisomers of asperphenamate la and patriscabratine 2a were achieved with a high yield,and total synthesis of 2a is firstly described here.The absolute configuration of patriscabratine was determined as(S,S).The compounds 1a-d and 2a-d have been tested by MTT assay in T47D,MDA-MB231,HL60,Hela and SGC-7901 cell lines in vitro.Among them,the(R,S)stereoisomer shows the strongest anticancer effects,while the(S,R)shows the weakest one.
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Received: 15 June 2009
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Corresponding Authors:
Tie Min Sun,E-mail address:suntiemin@126.com
E-mail: suntiemin@126.com
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