Anthracene based compounds as new L-type Ca2+ channel blockers: design, synthesis, and full biological profile

Journal of Medicinal Chemistry
Sergio BovaAlessandra Bisi

Abstract

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.

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Citations

Mar 8, 2013·Acta Crystallographica. Section E, Structure Reports Online·Barbara MiroslawMarta Struga
Jan 18, 2015·European Journal of Medicinal Chemistry·Alessandra BisiConcettina Cappadone
May 31, 2017·Vaccines·Christopher ConchaCristian Ibáñez

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