Mitochondria-targeting fluorescent molecules for high efficiency cancer growth inhibition and imaging.

ABSTRACT: Fluorescent mitochondria-accumulating delocalized lipophilic cations (DLCs) for cancer therapy have drawn significant attention in the field of cancer theranostics. One of the most promising fluorescent DLCs, F16, can selectively trigger the apoptosis and necrosis of cancer cells, making it an attractive targeted theranostic drug candidate. However, it suffers from low clinical translation potential, largely due to its inefficient anti-cancer activity (IC₅₀ in the μM range) and poorly understood structure-activity relationship (SAR). In this report, eleven indole-ring substituted F16 derivatives (F16s) were synthesized. Among these derivatives, 5BMF was identified as a highly effective theranostic agent, with in vitro studies showing a low IC₅₀ of ∼50 nM

SUBMITTER: Chen H 

PROVIDER: S-EPMC6836573 | biostudies-literature | 2019 Sep

REPOSITORIES: biostudies-literature