Guanidines: Synthesis of Novel Histamine H₃R Antagonists with Additional Breast Anticancer Activity and Cholinesterases Inhibitory Effect.

ABSTRACT: This study examines the properties of novel guanidines, designed and synthesized as histamine H₃R antagonists/inverse agonists with additional pharmacological targets. We evaluated their potential against two targets viz., inhibition of MDA-MB-231, and MCF-7 breast cancer cells viability and inhibition of AChE/BuChE. ADS10310 showed micromolar cytotoxicity against breast cancer cells, combined with nanomolar affinity at hH₃R, and may represent a promising target for the development of an alternative method of cancer therapy. Some of the newly synthesized compounds showed moderate inhibition of BuChE in the single-digit micromolar concentration ranges. H₃R antagonist with additional AChE/BuChE inhibitory effect might improve cognitive functions in Alz

SUBMITTER: Staszewski M 

PROVIDER: S-EPMC10223552 | biostudies-literature | 2023 Apr

REPOSITORIES: biostudies-literature