Tailored α-methylene-γ-butyrolactones and their effects on growth suppression in pancreatic carcinoma cells.
A selected series of racemic α-methylene-γ-butyrolactones (AMGBL) were synthesized via allylboration and screened against three human pancreatic cancer cell lines (Panc-1, MIA PaCa-2, and BxPC-3). This systematic study established a discernible relationship between the substitution pattern of AMGBL and their anti-proliferative activity. β,γ-diaryl-AMGBLs, particularly those with a trans-relationship exhibited higher potency than parthenolide and LC-1 against all three cell lines.
Ramachandran
P Veeraraghavan
PV
Department of Chemistry, Purdue University, 560 Oval Drive, West Lafayette, IN 47907-2084, United States. chandran@purdue.edu
Pratihar
Debarshi
D
Nair
Hari Narayanan G
HN
Walters
Matthew
M
Smith
Sadie
S
Yip-Schneider
Michele T
MT
Wu
Huangbing
H
Schmidt
C Max
CM
D015107:4-Butyrolactone / Q000737:chemistry / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects*; D045744:Cell Line, Tumor; D006801:Humans; D010190:Pancreatic Neoplasms / Q000473:pathology*
D015107:4-Butyrolactone