2. Academic Validation
  3. Design, synthesis and bioactivity evaluation of the combination of evodiamine and erlotinib linked by indolequinone

Design, synthesis and bioactivity evaluation of the combination of evodiamine and erlotinib linked by indolequinone

  • Bioorg Med Chem Lett. 2024 Jan 18:99:129619. doi: 10.1016/j.bmcl.2024.129619.
Binbin Wei 1,  Jingjing Ma 1,  Hui Guo 2,  Yuwei Wang 1,  Dongyan Guo 1,  Yuping Tang 3
Affiliations

Affiliations

  • 1 College of Pharmacy, Shaanxi Key Lab Basic & New Herbal Medicament Res, Shaanxi University of Chinese Medicine, Xian Yang, Shaanxi 712046, China.
  • 2 College of Pharmacy, Shaanxi Key Lab Basic & New Herbal Medicament Res, Shaanxi University of Chinese Medicine, Xian Yang, Shaanxi 712046, China. Electronic address: guohui@sntcm.edu.cn.
  • 3 College of Pharmacy, Shaanxi Key Lab Basic & New Herbal Medicament Res, Shaanxi University of Chinese Medicine, Xian Yang, Shaanxi 712046, China. Electronic address: yupingtang@sntcm.edu.cn.
PMID: 38244939 DOI: 10.1016/j.bmcl.2024.129619
Abstract

Compared with single-targeted therapy, the design and synthesis of heterozygous molecules is still a significant challenge for the discovery of antitumor drugs. Quinone oxidoreductase-1 (NQO1) is a potential target for selective Cancer therapy due to its overexpression in many Cancer cells and its unique bioredox properties. Based on the principle of combinatorial drug design, we successfully synthesized a new hybrid molecules 13 with an indolequinone structure. We found that the synthesized compounds exhibited much higher cytotoxicity against the tested Cancer cells than free drugs. Further mechanism studies confirmed that compound 13 induced cell Apoptosis was achieved by regulating p53-dependent mitochondrial pathway and cell cycle arrest at the G0/G1 phase.

Keywords

Biological activity; Erlotinib; Evodiamine; Indolequinone structure; Quinone oxidoreductase-1.

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