Synthetic I--(aminomethyl)-I3-butyrolactones and their anti-pancreatic cancer activities

Aminated I--methylene-I3-butyrolactones, which are readily synthesized with facile control of the diastereoisomerism, provide an economical and commercially-viable alternative to the use of aminated natural products. These aminoloactones, which exhibit excellent activity against three pancreatic can...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2013-12, Vol.23 (24), p.6911-6914
Main Authors: Ramachandran, P, Nicponski, Daniel, Nair, Hari, Helppi, Matthew, Gagare, Pravin, Schmidt, C, Yip-Schneider, Michele
Format: Article
Language:English
Subjects:
Pancreatic cancer
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Summary:Aminated I--methylene-I3-butyrolactones, which are readily synthesized with facile control of the diastereoisomerism, provide an economical and commercially-viable alternative to the use of aminated natural products. These aminoloactones, which exhibit excellent activity against three pancreatic cancer cell lines when measured at 10 mu MaPanc-1, MIA PaCa-2, and BxPC-3aand are comparable to or better than parthenolide and dimethylaminoparthenolide (DMAPT, LC-1). It has also been shown that there is an effect on the biological activity depending on the identity of the amine.
ISSN:0960-894X
DOI:10.1016/j.bmcl.2013.09.065