1. Academic Validation
  2. Identification of new hit to lead magmas inhibitors as potential therapeutics for glioblastoma

Identification of new hit to lead magmas inhibitors as potential therapeutics for glioblastoma

  • Bioorg Med Chem Lett. 2023 Jul 15:91:129330. doi: 10.1016/j.bmcl.2023.129330.
Bhaskar C Das 1 Javier J Lepe 2 Mohammed Adil Shareef 3 Naomi Lomeli 2 Sasmita Das 3 Daniela A Bota 4
Affiliations

Affiliations

  • 1 Arnold and Marie Schwartz College of Pharmacy and Health Sciences, Long Island University, Brooklyn, NY, USA; Department of Medicine and Pharmacological Sciences, Icahn School of Medicine at Mount Sinai, New York, NY 10029, USA.
  • 2 Department of Pathology and Laboratory Medicine, School of Medicine, University of California, Irvine, USA.
  • 3 Arnold and Marie Schwartz College of Pharmacy and Health Sciences, Long Island University, Brooklyn, NY, USA.
  • 4 Department of Pathology and Laboratory Medicine, School of Medicine, University of California, Irvine, USA; Department of Neurology, School of Medicine, University of California, Irvine, USA; Department of Neurological Surgery, School of Medicine, University of California, Irvine, USA; Chao Family Comprehensive Cancer Center, School of Medicine, University of California, Irvine, USA.
Abstract

In continuation of our previous efforts for the development of potent small molecules against brain Cancer, herein we synthesized seventeen new compounds and tested their anti-gliomapotential against established glioblastoma cell lines, namely, D54MG, U251, and LN-229 as well as patient derived cell lines (DB70 and DB93). Among them, the carboxamide derivatives, BT-851 and BT-892 were found to be the most active leads in comparison to our established hit compound BT#9.The SAR studies of our hit BT#9 compound resulted in the development of two new lead compounds by hit to lead strategy. The detailed biological studies are currently underway. The active compounds could possibly act as template for the future development of newer anti-glioma agents.

Keywords

Anti-glioma agents; Anticancer; Carboxamides; Glioblastoma; Hit to lead; Magmas protein; Oxadiazborole; Oxadiazoles.

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