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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.
- 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.)
- Subjects :
- 4-Butyrolactone chemical synthesis
4-Butyrolactone chemistry
4-Butyrolactone pharmacology
Amination
Antineoplastic Agents chemistry
Cell Line, Tumor
Cell Survival drug effects
Humans
Pancreatic Neoplasms metabolism
Pancreatic Neoplasms pathology
Sesquiterpenes chemistry
Sesquiterpenes toxicity
Stereoisomerism
Structure-Activity Relationship
4-Butyrolactone analogs & derivatives
Antineoplastic Agents chemical synthesis
Antineoplastic Agents pharmacology
Subjects
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