Exploring the Substitution of the C21-OAc Moiety in [11]Cytochalasans: Synthesis and Evaluation of Fluorophore Conjugates.

ABSTRACT: The actin cytoskeleton plays a central role in cellular organization and dynamics, yet the tools available for targeting actin function remain limited. Cytochalasans represent a large class of actin-targeting natural products that are readily cell permeable with varying cytotoxicity and actin-targeting capabilities in mammalian cells. Their pharmacologic exploitation not only requires an understanding of their mode of action but also exact knowledge of how they can be derivatized without affecting their bioactivity. Herein, the design, synthesis, and evaluation of five fluorescently labeled [11]cytochalasan derivatives generated from pyrichalasin H (PyriH) and 19,20-epoxycytochalasin C (EpoxyCytoC) are reported. Guided by molecular docking, the C21-OAc moiety is identified as a promising s

SUBMITTER: Kagho MD 

PROVIDER: S-EPMC12781145 | biostudies-literature | 2026 Jan

REPOSITORIES: biostudies-literature