Synonyms: GS-6615 | GS6615
Compound class:
Synthetic organic
Comment: Eleclazine is a sodium channel inhibitor, modulating cardiac late Na+ currents via the Nav1.5 (gene symbol SCN5A) channel. The compound is a dihydrobenzodiazepine type structure. Dihydrobenzodiazepine scaffolds are being developed as α-helix mimetics, with the potential to inhibit protein-protein interactions [1,3-5]. This chemical structure and its use is covered by patent US20150038489 [2].
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References |
1. Antuch W, Menon S, Chen QZ, Lu Y, Sakamuri S, Beck B, Schauer-Vukasinović V, Agarwal S, Hess S, Dömling A. (2006)
Design and modular parallel synthesis of a MCR derived alpha-helix mimetic protein-protein interaction inhibitor scaffold. Bioorg Med Chem Lett, 16 (6): 1740-3. [PMID:16427279] |
2. Belardinelli L, Rajamani S, Zeng D. (2015)
Compound and methods for treating long qt syndrome. Patent number: US20150038489 A1. Assignee: Gilead Sciences, Inc.. Priority date: 01/08/2013. Publication date: 05/02/2015. |
3. Cummings MD, Schubert C, Parks DJ, Calvo RR, LaFrance LV, Lattanze J, Milkiewicz KL, Lu T. (2006)
Substituted 1,4-benzodiazepine-2,5-diones as alpha-helix mimetic antagonists of the HDM2-p53 protein-protein interaction. Chem Biol Drug Des, 67 (3): 201-5. [PMID:16611213] |
4. Grasberger BL, Lu T, Schubert C, Parks DJ, Carver TE, Koblish HK, Cummings MD, LaFrance LV, Milkiewicz KL, Calvo RR et al.. (2005)
Discovery and cocrystal structure of benzodiazepinedione HDM2 antagonists that activate p53 in cells. J Med Chem, 48 (4): 909-12. [PMID:15715460] |
5. Raboisson P, Marugán JJ, Schubert C, Koblish HK, Lu T, Zhao S, Player MR, Maroney AC, Reed RL, Huebert ND et al.. (2005)
Structure-based design, synthesis, and biological evaluation of novel 1,4-diazepines as HDM2 antagonists. Bioorg Med Chem Lett, 15 (7): 1857-61. [PMID:15780621] |