A chiral trimethyl lock based on the vicinal disubstituent effect: prolonged release of camptothecin into cancer cells.
Silvia VenturiFerdinando ChiaradonnaFrancesco G GattiBarbara La FerlaRoberta PaloriniBarbara ZerbatoPublished in: Chemical communications (Cambridge, England) (2024)
Synthesis and in vitro testing of a prodrug designed for the controlled delivery of the anticancer drug camptothecin within pancreatic cancer cells are reported. Our study reveals a non-conventional pharmacokinetic release characterized by an exponential pattern before reaching the half-life ( t 1/2 ) and a linear pattern thereafter. The release mechanism was triggered either by hydrolytic enzymes and/or by the acid microenvironment of cancer cells.