New Diarylamine K_V10.1 Inhibitors and Their Anticancer Potential.

ABSTRACT: Expression of the voltage-gated potassium channel K_V10.1 (Eag1) has been detected in over 70% of human cancers, making the channel a promising new target for new anticancer drug discovery. A new structural class of K_V10.1 inhibitors was prepared by structural optimisation and exploration of the structure-activity relationship of the previously published hit compound ZVS-08 (1) and its optimised analogue 2. The potency and selectivity of the new inhibitors between K_V10.1 and hERG were investigated using whole-cell patch-clamp experiments. We obtained two new optimised K_V10.1 inhibitors, 17a and 18b, with improved nanomolar IC₅₀ values of 568 nM and 214 nM, respectively. Compound 17a exhibited better ra

SUBMITTER: Gubic S 

PROVIDER: S-EPMC9501377 | biostudies-literature | 2022 Sep

REPOSITORIES: biostudies-literature