Recent advances in the discovery of small molecules targeting glioblastoma

Author(s)

dos Santos Fernandes, Guilherme Felipe ^{[1, 2]} ; Fernandes, Barbara Colatto ^[1] ; Valente, Valeria ^[1] ; dos Santos, Jean Leandro ^{[1, 2]}

Affiliation

^[1] Sao Paulo State Univ UNESP, Sch Pharmaceut Sci, BR-14800903 Araraquara - Brazil

^[2] Sao Paulo State Univ UNESP, Inst Chem, BR-14800060 Araraquara - Brazil

• Document type: Review article
• Source: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY; v. 164, p. 8-26, FEB 15 2019.
• Web of Science Citations: 3

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. (C) 2018 Elsevier Masson SAS. All rights reserved. (AU)

• FAPESP's process: 18/11079-0 - Synthesis and antitubercular activity of new N-oxide compounds designed to treat multiresistant-tuberculosis
• Grantee: Jean Leandro dos Santos
• Support Opportunities: Regular Research Grants
• FAPESP's process: 16/09502-7 - Design, synthesis and antitubercular activity of new oxazolidinones useful for the treatment of multidrug-resistant tuberculosis
• Grantee: Guilherme Felipe dos Santos Fernandes
• Support Opportunities: Scholarships in Brazil - Doctorate