2. Academic Validation
  3. Chemistry and biology of ophiobolin A and its congeners

Chemistry and biology of ophiobolin A and its congeners

  • Bioorg Med Chem Lett. 2019 Apr 1;29(7):859-869. doi: 10.1016/j.bmcl.2019.02.007.
Marco Masi 1,  Ramesh Dasari 2,  Antonio Evidente 1,  Veronique Mathieu 3,  Alexander Kornienko 4
Affiliations

Affiliations

  • 1 Dipartimento di Scienze Chimiche, Università di Napoli Federico II, Complesso Universitario Monte Sant'Angelo, Via Cintia 4, 80126 Napoli, Italy.
  • 2 Department of Chemistry and Biochemistry, Texas State University, San Marcos, TX 78666, USA.
  • 3 Department of Pharmacotherapy and Pharmaceutics, Faculté de Pharmacie, Université Libre de Bruxelles (ULB), Brussels, Belgium; dULB Cancer Research Center, Université Libre de Bruxelles, Brussels, Belgium.
  • 4 Department of Chemistry and Biochemistry, Texas State University, San Marcos, TX 78666, USA; Department of Chemistry, North Caucasus Federal University, 1a Pushkin St, Stavropol 355009, Russian Federation.
PMID: 30765189 DOI: 10.1016/j.bmcl.2019.02.007
Abstract

Ophiobolin A is a Fungal secondary metabolite that was found to have significant activity against apoptosis-resistant glioblastoma cells through the induction of a non-apoptotic cell death, offering an innovative strategy to combat this aggressive Cancer. The current article aims to make the bridge between the anti-cancer effects of ophiobolin A and its unique reaction with primary amines and suggests that pyrrolylation of lysine residues on its intracellular target protein(s) and/or phosphatidylethanolamine lipid is responsible for its biological effects. The article also discusses chemical derivatization of ophiobolin A to establish first synthetically generated structure-activity relationship. Finally, the reported total synthesis efforts toward the ophiobolin class of sesterterpenes are discussed and identified as a fertile area for improvement in pursuit of these molecules as Anticancer agents.

Keywords

Anticancer activity; Apoptosis resistance; Glioblastoma; Ophiobolin A; Sesterterpenes.

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