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

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.

SUBMITTER: Das BC

PROVIDER: S-EPMC10506439 | biostudies-literature | 2023 Jul

REPOSITORIES: biostudies-literature

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

Das Bhaskar C BC Lepe Javier J JJ Adil Shareef Mohammed M Lomeli Naomi N Das Sasmita S Bota Daniela A DA

Bioorganic & medicinal chemistry letters 20230516

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 ...[more]

PMID: 37201660

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