2. Academic Validation
  3. Indole: A privileged scaffold for the design of anti-cancer agents

Indole: A privileged scaffold for the design of anti-cancer agents

  • Eur J Med Chem. 2019 Dec 1:183:111691. doi: 10.1016/j.ejmech.2019.111691.
Yichao Wan 1,  Yuanhua Li 2,  Chunxing Yan 2,  Mi Yan 3,  Zilong Tang 4
Affiliations

Affiliations

  • 1 Key Laboratory of Theoretical Organic Chemistry and Functional Molecule, Ministry of Education, Hunan Provincial Key Laboratory of Controllable Preparation and Functional Application of Fine Polymers, School of Chemistry and Chemical Engineering, Hunan University of Science and Technology, Xiangtan, Hunan, 411201, PR China; Hunan Provincial College Key Laboratory of QSAR/QSPR, Hunan Provincial Key Lab of Advanced Materials for New Energy Storage and Conversion, Hunan University of Science and Technology, Xiangtan, Hunan, 411201, PR China. Electronic address: 07wanyichao@hnust.edu.cn.
  • 2 Key Laboratory of Theoretical Organic Chemistry and Functional Molecule, Ministry of Education, Hunan Provincial Key Laboratory of Controllable Preparation and Functional Application of Fine Polymers, School of Chemistry and Chemical Engineering, Hunan University of Science and Technology, Xiangtan, Hunan, 411201, PR China; Hunan Provincial College Key Laboratory of QSAR/QSPR, Hunan Provincial Key Lab of Advanced Materials for New Energy Storage and Conversion, Hunan University of Science and Technology, Xiangtan, Hunan, 411201, PR China.
  • 3 Department of Pharmacy, The Second Hospital of Shandong University, Jinan, Shandong, 250033, PR China.
  • 4 Key Laboratory of Theoretical Organic Chemistry and Functional Molecule, Ministry of Education, Hunan Provincial Key Laboratory of Controllable Preparation and Functional Application of Fine Polymers, School of Chemistry and Chemical Engineering, Hunan University of Science and Technology, Xiangtan, Hunan, 411201, PR China; Hunan Provincial College Key Laboratory of QSAR/QSPR, Hunan Provincial Key Lab of Advanced Materials for New Energy Storage and Conversion, Hunan University of Science and Technology, Xiangtan, Hunan, 411201, PR China. Electronic address: zltang@hnust.edu.cn.
PMID: 31536895 DOI: 10.1016/j.ejmech.2019.111691
Abstract

In general, heterocyclic compounds are a significant source of pharmacologically active compounds. Among them, the indole scaffold widely distributes in Natural Products and bioactive molecules including anti-cancer agents. In view of its unique physic-chemical and biological properties, it has been used as a privileged scaffold in the anti-cancer agents design. So far, many natural and synthetic indole derivatives have been discovered as promising anti-cancer agents used in clinic or clinical evaluations, suggesting its prominent place in anti-cancer drugs development. This review aimed to provide a clear knowledge on the recent development of indoles as anti-cancer agents, such as myeloid cell leukemia-1 (Mcl-1) inhibitors, proviral insertion site in moloney murine leukemia virus (Pim) inhibitors, histone deacetylase (HDAC) inhibitors, silent mating type information regulation 2 homolog (SIRT) inhibitors and tubulin inhibitors, and made an insight into the corresponding structure-activity relationships (SARs). We hope the review could give a guide to develop new anti-cancer agents with greater potency against drug-sensitive and drug-resistant cancers in the future.

Keywords

Anti-Cancer; Drug design; Indole; Structure-activity relationships.

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