Adamantane-Quinoxalone Hybrids: Precision Chemotypes and Their Molecular Mechanisms in Acute Myeloid Leukemia

Acute myeloid leukemia (AML) is an aggressive blood cancer with a poor prognosis, especially when diagnosed late. Around 10-15% of cases involve the specific chromosomal abnormality t(8;21), which drives uncontrolled myeloid cell proliferation and contributes to disease onset. Despite advances in AML research and treatment protocols, outcomes for t(8;21) AML remain stagnant, as patients receive standard, nonspecific chemotherapies. This one-size-fits-all approach targets both cancerous and healthy cells, leading to unwanted toxicity and highlighting the urgent need for targeted therapies. In this study, we present a precision chemotype based on a quinoxalone-tethered adamantane framework developed via a metal- and light-free protocol. The compound selectively inhibits t(8;21) AML cell proliferation and induces cell death by disrupting growth and metabolic pathways, as demonstrated through bioassays, RNA sequencing, and proteomic analysis. Notably, it spares other leukemic and solid cancer cells, underscoring its specificity and potential as a targeted therapy for t(8;21) AML.

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Publication Details

Journal
Journal of Medicinal Chemistry
Published
2025-03-31
DOI
https://doi.org/10.1021/acs.jmedchem.5c00262
Citations
9
Primary Topic
Synthesis and Biological Evaluation
Type
article
Field-Weighted Citation Impact
8.42

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article

Adamantane-Quinoxalone Hybrids: Precision Chemotypes and Their Molecular Mechanisms in Acute Myeloid Leukemia

Vibhor Kumar, Sangita Dattatray Shinde, Sai Swetha Uppalapati, Ambika Chamoli et al.
9 citations
Journal of Medicinal Chemistry
Synthesis and Biological Evaluation
8.42
article

Adamantane-Quinoxalone Hybrids: Precision Chemotypes and Their Molecular Mechanisms in Acute Myeloid Leukemia

Vibhor Kumar, Sangita Dattatray Shinde, Sai Swetha Uppalapati, Ambika Chamoli, Dinesh Kumar, J.C. Sharma, Amit Mandoli
article en
9 citations

Abstract

Acute myeloid leukemia (AML) is an aggressive blood cancer with a poor prognosis, especially when diagnosed late. Around 10-15% of cases involve the specific chromosomal abnormality t(8;21), which drives uncontrolled myeloid cell proliferation and contributes to disease onset. Despite advances in AML research and treatment protocols, outcomes for t(8;21) AML remain stagnant, as patients receive standard, nonspecific chemotherapies. This one-size-fits-all approach targets both cancerous and healthy cells, leading to unwanted toxicity and highlighting the urgent need for targeted therapies. In this study, we present a precision chemotype based on a quinoxalone-tethered adamantane framework developed via a metal- and light-free protocol. The compound selectively inhibits t(8;21) AML cell proliferation and induces cell death by disrupting growth and metabolic pathways, as demonstrated through bioassays, RNA sequencing, and proteomic analysis. Notably, it spares other leukemic and solid cancer cells, underscoring its specificity and potential as a targeted therapy for t(8;21) AML.

Journal of Medicinal ChemistryVol. 68(7)
Indraprastha Institute of Information Technology Delhi (IN), National Institute of Pharmaceutical Education and Research - Ahmedabad (IN)
National Institute of Pharmaceutical Education and Research, Ahmedabad, Indian Council of Medical Research, Department of Pharmaceuticals, Ministry of Chemicals and Fertilizers, India, Science and Engineering Research Board
Openalex Percentile: Top 2%
Synthesis and Biological Evaluation
8.42
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