Anthracene Based Compounds as New L-type Ca~2+ Channel Blockers: Design, Synthesis, and Full Biological Profile

摘要

L-Type Ca~2+ channels (LTCCs) play a key role in the regulation of vascular smooth muscle contraction, and substances that interfere with their function (Ca~2+ channel blockers) are widely used in the therapy of hypertension. Here, we report anthracene_maleimide derivatives as new LTCC blockers. Among these, 3, lacking intracellular effects, was investigated in more detail. The results show that 3 binds preferentially to inactivated LTCCs, directly interacting with the pore-forming subunit of the channel.