Identification of New Hit to Lead Magmas Inhibitors As Potential Therapeutics for Glioblastoma

Overview

Journal Bioorg Med Chem Lett

Specialty Biochemistry

Date 2023 May 18

PMID 37201660

Authors

Bhaskar C Das

Javier J Lepe

Mohammed Adil Shareef

Naomi Lomeli

Sasmita Das

Daniela A Bota

Affiliations

Soon will be listed here.

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.

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