Factors influencing the cytotoxicity of α-methylene-γ-hydroxy esters against pancreatic cancer. Issue 19 (1st October 2015)

• Record Type: Journal Article
• Authors: Ramachandran, P. Veeraraghavan; Helppi, Matthew A.; Lehmkuhler, Arlie L.; Marchi, Jennifer M.; Schmidt, C. Max; Yip-Schneider, Michele T.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 25:Issue 19(2015)
• Page Start: 4270
• Page End: 4273
• Publication Date: 2015-10-01
• Subjects: Pancreatic -- Pro-drug -- Lactonization -- Cytotoxicity -- Hydroxy esters; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.07.087
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: A systematic study to identify the factors influencing the cytotoxicity of α-methylene-γ-hydroxy esters against three pancreatic cancer cell lines (Panc-1, MIA-PaCa-2, and BxPC-3) has established that, in addition to Michael acceptor abilities, the possibility to lactonize to α-methylene-γ-butyrolactones is as important. The substitution pattern and the number of carbons between the hydroxy and ester moieties also influence the bio-activity.