1. Academic Validation
  2. New bioluminescent coelenterazine derivatives with various C-6 substitutions

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

Affiliations

  • 1 Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmaceutical Sciences, Shandong University, Jinan, Shandong 250012, China. mli@sdu.edu.cn.
  • 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.
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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