Synthesis, binding assays, cytotoxic activity and docking studies of benzimidazole and benzothiophene derivatives with selective affinity for the CB2 cannabinoid receptor
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- 作者：Javier Romero-Parraa ; Jaime Mella-Raipá ; nb ; Vittoria Palmieric ; Marco Allarà ; c ; Maria Jose Torresa ; Herná ; n Pessoa-Mahanad ; Patricio Iturriaga-Vá ; squeze ; Rossy Escobara ; Mario Faú ; ndeza ; Vincenzo Di Marzoc ; C. David Pessoa-Mahanaa ; dvdpss91@gmail.com" class="auth_mail" title="E-mail the corresponding author
- 关键词：Cannabinoids ; Benzimidazole ; Benzothiophene ; Binding ; HL-60 cells ; Cytotoxicity studies ; Docking assays
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：29 November 2016
- 年：2016
- 卷：124
- 期：Complete
- 页码：17-35
- 全文大小：2046 K
文摘
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Benzimidazoles were more selective for CB2 cannabinoid receptor than benzothiophenes derivatives.
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The compounds were selective and cytotoxic for HL-60 cells.
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An interaction of the molecules with Lys109 would be responsible for CB2 receptor selectivity.
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Compound 8f displayed low Ki CB2 and low EC50 in HL-60 cells as well as no toxic effect in VERO non-neoplastic cells.