1. Academic Validation
  2. Recent advances in the discovery of small molecules targeting glioblastoma

Recent advances in the discovery of small molecules targeting glioblastoma

  • Eur J Med Chem. 2019 Feb 15:164:8-26. doi: 10.1016/j.ejmech.2018.12.033.
Guilherme Felipe Dos Santos Fernandes 1 Barbara Colatto Fernandes 2 Valeria Valente 2 Jean Leandro Dos Santos 3
Affiliations

Affiliations

  • 1 São Paulo State University (UNESP), School of Pharmaceutical Sciences, Araraquara, 14800-903, Brazil; São Paulo State University (UNESP), Institute of Chemistry, Araraquara, 14800-060, Brazil.
  • 2 São Paulo State University (UNESP), School of Pharmaceutical Sciences, Araraquara, 14800-903, Brazil.
  • 3 São Paulo State University (UNESP), School of Pharmaceutical Sciences, Araraquara, 14800-903, Brazil; São Paulo State University (UNESP), Institute of Chemistry, Araraquara, 14800-060, Brazil. Electronic address: jean.santos@unesp.br.
Abstract

Glioblastoma (GBM) is one of the most common central nervous system cancers. It is characterized as a fast-growing tumor that arises from multiple cell types with neural stem-cell-like properties. Additionally, GBM tumors are highly invasive, which is attributed to the presence of glioblastoma stem cells that makes surgery ineffective in most cases. Currently, temozolomide is the unique chemotherapy option approved by the U.S. Food and Drug Administration for GBM treatment. This review analyzes the emergence and development of new synthetic small molecules discovered as promising anti-glioblastoma agents. A number of compounds were described herein and grouped according to the main chemical class used in the drug discovery process. Importantly, we focused only on synthetic compounds published in the last 10 years, thus excluding Natural Products. Furthermore, we included in this review only those most biologically active compounds with proven in vitro and/or in vivo efficacy.

Keywords

Cancer; Drug discovery; Glioblastoma; Medicinal chemistry; New compounds.

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