Journal
ACS COMBINATORIAL SCIENCE
Volume 13, Issue 2, Pages 147-153Publisher
AMER CHEMICAL SOC
DOI: 10.1021/co1000458
Keywords
diversity-oriented synthesis; dipeptide mimetic compounds; bioactive molecular skeletons; microwave-assisted reactions
Funding
- Natural Science Foundation of China [21002083, 21072163]
- Natural Science Foundation [09KJB150011]
- Jiangsu Education Committee [08QL001]
- Xuzhou Normal University [09XKXK01]
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The diversity-oriented synthesis of dipeptide mimetic compounds embedded with bioactive molecular skeletons have been successfully established via microwave-assisted reactions between various 4-arylidene-2-phenyloxazol-5(4H)-ones and a broad scope of amines including aliphatic, aromatic, and heteroaromatic ones. This synthetic approach has prominent features of short reaction time, high yields, operational simplicity,as well as widespread applications, leading to a facile and straightforward access to structurally diverse dipeptide analogues with, potential bioactivities, Moreover, the preliminary evaluation on the cytotoxic activity of this type-of dipeptide derivatives has resulted in the finding of five Compounds with stronger cytotoxicity than doxorubicin hydrochloride at the concentration of 10 mu g/mL.
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