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Synthetic α-(aminomethyl)-γ-butyrolactones and their anti-pancreatic cancer activities.

Synthetic α-(aminomethyl)-γ-butyrolactones and their anti-pancreatic cancer activities.

Authors :
Ramachandran PV
Nicponski DR
Nair HN
Helppi MA
Gagare PD
Schmidt CM
Yip-Schneider MT
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2013 Dec 15; Vol. 23 (24), pp. 6911-4. Date of Electronic Publication: 2013 Sep 30.
Publication Year :
2013

Abstract

Aminated α-methylene-γ-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 μM-Panc-1, MIA PaCa-2, and BxPC-3-and 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.<br /> (Copyright © 2013 Elsevier Ltd. All rights reserved.)

Details

Language :
English
ISSN :
1464-3405
Volume :
23
Issue :
24
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
24176399
Full Text :
https://doi.org/10.1016/j.bmcl.2013.09.065