Anthracene Based Compounds as New L-type Ca2+ Channel Blockers: Design, Synthesis, and Full Biological Profile

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• 作者：Sergio Bova^† ; ; Simona Saponara^‡ ; ; Angela Rampa^§ ; ; Silvia Gobbi^§ ; ; Lorenzo Cima^† ; ; Fabio Fusi^‡ ; ; Giampietro
• 刊名：Journal of Medicinal Chemistry
• 出版年：2009
• 出版时间：March 12, 2009
• 年：2009
• 卷：52
• 期：5
• 页码：1259-1262
• 全文大小：156K
• 年卷期：v.52,no.5(March 12, 2009)
• ISSN：1520-4804

文摘

L-Type Ca²⁺ channels (LTCCs) play a key role in the regulation of vascular smooth muscle contraction, and substances that interfere with their function (Ca²⁺ 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.