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

Bhaskar C. Das; Javier J. Lepe; Mohammed Adil Shareef; Naomi Lomeli; Sasmita Das; Daniela A. Bota

doi:10.1016/j.bmcl.2023.129330

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

Bhaskar C. Das
, Javier J. Lepe
, Mohammed Adil Shareef
, Naomi Lomeli
, Sasmita Das
, Daniela A. Bota

Pharmaceutical Sciences

University of California at Irvine
Long Island University

Research output: Contribution to journal › Article › peer-review

1 Scopus citations

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.

Original language	English
Article number	129330
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	91
DOIs	https://doi.org/10.1016/j.bmcl.2023.129330
State	Published - Jul 15 2023

Keywords

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

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10.1016/j.bmcl.2023.129330

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title = "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.",

keywords = "Anti-glioma agents, Anticancer, Carboxamides, Glioblastoma, Hit to lead, Magmas protein, Oxadiazborole, Oxadiazoles",

author = "Das, \{Bhaskar C.\} and Lepe, \{Javier J.\} and \{Adil Shareef\}, Mohammed and Naomi Lomeli and Sasmita Das and Bota, \{Daniela A.\}",

note = "Publisher Copyright: {\textcopyright} 2023",

year = "2023",

month = jul,

day = "15",

doi = "10.1016/j.bmcl.2023.129330",

language = "English",

volume = "91",

journal = "Bioorganic and Medicinal Chemistry Letters",

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TY - JOUR

T1 - Identification of new hit to lead magmas inhibitors as potential therapeutics for glioblastoma

AU - Das, Bhaskar C.

AU - Lepe, Javier J.

AU - Adil Shareef, Mohammed

AU - Lomeli, Naomi

AU - Das, Sasmita

AU - Bota, Daniela A.

PY - 2023/7/15

Y1 - 2023/7/15

N2 - 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.

AB - 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.

KW - Anti-glioma agents

KW - Anticancer

KW - Carboxamides

KW - Glioblastoma

KW - Hit to lead

KW - Magmas protein

KW - Oxadiazborole

KW - Oxadiazoles

UR - https://www.scopus.com/pages/publications/85162098641

U2 - 10.1016/j.bmcl.2023.129330

DO - 10.1016/j.bmcl.2023.129330

M3 - Article

C2 - 37201660

AN - SCOPUS:85162098641

SN - 0960-894X

VL - 91

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

M1 - 129330

ER -

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

Abstract

Keywords

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