4-(5-Fluoropyridin-2-yl)-2azetidinones to Fight Against Drug-Resistant Pancreatic Cancer
Description
The present technology consists of compounds that demonstrate outstanding results against drug-resistant cancer cell lines.
Problem
Around 95% of pancreatic tumors are driven by mutations in KRAS gene, subbed “undruggable” and prevalent in 5 drug-resistant pancreatic cancers. Currently, there is no effective medicine in the market for drug-resistant cancers.
Solution
6 potent anti-pancreatic cancer 2-azetidinone molecules against drug-resistant cell lines were designed, validated in silico, synthesized through multi-step process, and conducted in vitro anti-pancreatic cancer evaluation (2D-culture & 3D-tumorsphere formation assays). The series consists of 12 small molecules.
Value Proposition
These derivatives of compounds show excellent cytotoxicity against drug-resistant pancreatic cancer cell lines (PANC-1 cells): Best IC50 values in 2D-culture and 3D-tumorsphere assays are 2.55 nM and 2.33 nM, respectivelyCompetitive Advantages
- 3 to 359 times more selective towards PANC-1 cells compared to normal pancreatic ductal epithelial cells
- Potential antibacterial and drug-resistant antibacterial activity against various types of infections
Status of Development
Prototype is near commercial grade, and has been tested in an operational lab environment
IP Status
- Patent WO 2019227040
- Licensing Available
