Exploring diarylheptanoid derivatives to target LIMK1 as potential agents against colorectal cancer.

ABSTRACT: LIMK1 has been demonstrated to be highly correlated with the progression and overall survival rates of colorectal cancer (CRC) patients. In this study, a series of diarylheptanoid scaffold derivatives were intentionally designed and synthesised to evaluate their potential as LIMK1 inhibitors. Among these compounds, compounds 13a and XV exhibited LIMK1 inhibitory activity with IC₅₀ values of 0.94 and 0.57 µM, respectively. We also disclosed the structure-activity relationship of the resulting compounds that exhibited LIMK1 inhibition. Catechol-containing diarylheptanoid was identified as a promising scaffold for LIMK1 inhibitors. Notably, compound 13a demonstrated selectivity in inhibiting the tyrosine kinase-like family and exhibited potent inhibition of CRC

SUBMITTER: Chen LC 

PROVIDER: S-EPMC12624955 | biostudies-literature | 2025 Dec

REPOSITORIES: biostudies-literature