Anticancer Properties of Novel 4‐methylene‐1,2‐diphenylpyrazolidin‐3‐ones |
| |
| Authors: | Katarzyna Gach Jacek Szymański Dorota Pomorska Angelika D?ugosz Jakub Modranka Marlena Michalak Tomasz Janecki Anna Janecka |
| |
| Institution: | 1. Department of Biomolecular Chemistry, Faculty of Medicine, Medical University of Lodz, Mazowiecka 6/8, Lodz, Poland;2. Central Scientific Laboratory, Division of Public Health, Faculty of Health Sciences, Medical University of Lodz, Mazowiecka 6/8, Lodz, Poland;3. Institute of Organic Chemistry, Lodz University of Technology, ?eromskiego 116, Lodz, Poland |
| |
| Abstract: | The limited success of the currently used antitumor therapies is the driving force for organic chemists to seek new lead structures with anticancer potential. Two α‐methylene‐γ‐lactams with an additional nitrogen atom in the lactam ring, 5‐vinyl‐1,2‐diphenyl‐4‐methylenepyrazolidin‐3‐one ( 2a ) and 5‐phenyl‐1,2‐diphenyl‐4‐methylenepyrazolidin‐3‐one ( 2b ) have been synthesized. Their anticancer activity was assessed in MCF‐7 cells. Both compounds inhibited cell proliferation and induced DNA damage and apoptosis, with 2a being the more potent analog. Synergistic effects of 2a used in combination with known anticancer drugs, 5‐fluorouracil, taxol, and oxaliplatin were evaluated. Compound 2a significantly enhanced the antitumor action of oxaliplatin and 5‐fluorouracil, but not taxol. |
| |
| Keywords: | anticancer drugs apoptosis breast cancer cell proliferation DNA damage α ‐Methylene‐γ ‐lactams |
|
|
