New bioluminescent coelenterazine derivatives with various C-6 substitutions

  • Org Biomol Chem. 2017 Aug 23;15(33):7008-7018. doi: 10.1039/c7ob01554b.
Tianyu Jiang  1 ,  Xingye Yang  1 ,  Yubin Zhou  2 ,  Ilia Yampolsky  3 ,  Lupei Du  1 ,  Minyong Li  1
Affiliations
  • 1. Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmaceutical Sciences, Shandong University, Jinan, Shandong 250012, China. [email protected].
  • 2. Center for Translational Cancer Research, Institute of Biosciences and Technology, College of Medicine, Texas A&M University, Houston, TX 77030, USA.
  • 3. Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry of the Russian Academy of Sciences, Miklukho-Maklaya, 16/10, Moscow 117997, Russia and Pirogov Russian National Research Medical University, Ostrovitianov 1, Moscow 117997, Russia.
PMID: 28795755 DOI: 10.1039/c7ob01554b
Abstract

A series of new coelenterazine analogs with varying substituents at the C-6 position of the imidazopyrazinone core have been designed and synthesized for the extension of bioluminescence substrates. Some of them display excellent bioluminescence properties compared to DeepBlueC™ or native coelenterazine with both in vitro and in vivo biological evaluations, thus placing these derivatives among the most ideal substrates for Renilla bioluminescence applications.

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