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. Epub 2018 Dec 16.

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.

Publication types

  • Review

MeSH terms

  • Animals
  • Central Nervous System Neoplasms / drug therapy
  • Drug Discovery
  • Glioblastoma / drug therapy*
  • Humans
  • Neoplastic Stem Cells / drug effects
  • Neoplastic Stem Cells / pathology