Back to Search
Start Over
Dichloroacetyl Amides of 3,5-Bis(benzylidene)-4-piperidones Displaying Greater Toxicity to Neoplasms than to Non-Malignant Cells.
- Source :
- Medicines; Jun2022, Vol. 9 Issue 6, p1-11, 11p
- Publication Year :
- 2022
-
Abstract
- A series of 3,5-bis(benzylidene)-1-dichloroacetyl-4-piperidones 1a-l was evaluated against Ca9-22, HSC-2, HSC-3, and HSC-4 squamous cell carcinomas. Virtually all of the compounds displayed potent cytotoxicity, with 83% of the CC<subscript>50</subscript> values being submicromolar and several CC<subscript>50</subscript> values being in the double digit nanomolar range. The compounds were appreciably less toxic to human HGF, HPLF, and HPC non-malignant cells, which led to some noteworthy selectivity index (SI) figures. From these studies, 1d,g,k emerged as the lead molecules in terms of their potencies and SI values. A Quantitative Structure-Activity Relationship (QSAR) study revealed that cytotoxic potencies and potency-selectivity expression figures increased when the magnitude of the sigma values in the aryl rings was elevated. The modes of action of the representative cytotoxins in Ca9-22 cells were found to include G2/M arrest and stimulation of the cells to undergo mitosis and cause poly(ADP-ribose) polymerase (PARP) and procaspase 3 cleavage. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 23056320
- Volume :
- 9
- Issue :
- 6
- Database :
- Complementary Index
- Journal :
- Medicines
- Publication Type :
- Academic Journal
- Accession number :
- 157981916
- Full Text :
- https://doi.org/10.3390/medicines9060035