A chiral trimethyl lock based on the disubstituent effect: prolonged release of camptothecin into cancer cells

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...

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Published inChemical communications (Cambridge, England) Vol. 6; no. 51; pp. 6524 - 6527
Main Authors Venturi, Silvia, Chiaradonna, Ferdinando, Gatti, Francesco G, La Ferla, Barbara, Palorini, Roberta, Zerbato, Barbara
Format Journal Article
Published 20.06.2024
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Summary: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. A camptothecin prodrug with a non-conventional prolonged release based on chiral-TML was synthesised and evaluated.
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Electronic supplementary information (ESI) available: Experimental procedures, compound characterization, copies of
https://doi.org/10.1039/d4cc01220h
H-NMR and
C-NMR spectra, progress curves and linear regressions of the kinetic study. See DOI
ISSN:1359-7345
1364-548X
DOI:10.1039/d4cc01220h