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|Title:||Anthracene based compounds as new L-type Ca2+ channel blockers: design, synthesis, and full biological profile||Authors:||Bova, S
Sgaragli, GIAN PIETRO
DE LOS RIOS, C
|Issue Date:||2009||Project:||None||Journal:||JOURNAL OF MEDICINAL CHEMISTRY||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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