First-in-Class Colchicine-Based Visible Light Photoswitchable Microtubule Dynamics Disrupting Agent.

ABSTRACT: Compounds that disrupt microtubule dynamics, such as colchicine, paclitaxel, or Vinca alkaloids, have been broadly used in biological studies and have found application in clinical anticancer medications. However, their main disadvantage is the lack of specificity towards cancerous cells, leading to severe side effects. In this paper, we report the first synthesis of 12 new visible light photoswitchable colchicine-based microtubule inhibitors AzoCols. Among the obtained compounds, two photoswitches showed light-dependent cytotoxicity in cancerous cell lines (HCT116 and MCF-7). The most promising compound displayed a nearly twofold increase in potency. Moreover, dissimilar inhibition of purified tubulin polymerisation in cell-free assay and light-dependent disruption of microtubule o

SUBMITTER: Borys F 

PROVIDER: S-EPMC10378023 | biostudies-literature | 2023 Jul

REPOSITORIES: biostudies-literature