Blue Fluorescent Siloxytecans Exhibit Potent Anticancer Activity and Enable Direct Real-Time Quantification of Intracellular Uptake.

ABSTRACT: Notwithstanding the natural abundance of silicon on Earth, silicon-containing compounds comprise relatively few pharmaceutical drugs, though several silylated natural products have demonstrated greater bioavailability and lipophilicity. Here, we apply this strategy in the preparation and biological evaluation of synthetic camptothecin analogs involving a C-10 silyl ether on SN-38, which not only blocks a site of metabolism but also enhances bright-blue fluorescence properties in such compounds. These siloxytecans exhibit comparable dose- and time-dependent antiproliferative activity in a broad panel of cancer cells. Uniquely, we demonstrate that the enhanced fluorescence of these compounds enables real-time, quantitative visualization of the dynamics and selectivity of intracellular uptake

SUBMITTER: Lo I 

PROVIDER: S-EPMC12921511 | biostudies-literature | 2026 Feb

REPOSITORIES: biostudies-literature