ArticleEuropean journal of medicinal chemistry2023
Design, synthesis, and biological activity of dual monoamine oxidase A and heat shock protein 90 inhibitors, N-Methylpropargylamine-conjugated 4-isopropylresorcinol for glioblastoma.
Article in European journal of medicinal chemistry, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed, 16 citations in OpenAlex.
- Tasimelteon inhibits glioma proliferation by inducing ferroptosis via the SP1/ACSL4 pathway.Cellular oncology (Dordrecht, Netherlands) · 2026Article
- Recent progress in the development of HSP90 inhibitors: structure-activity relationship and biological evaluation studies.Molecular diversity · 2026Review
- Dual MAO A and HSP90 inhibitors enhance anti-PD-1 therapy and suppress colorectal cancer.Frontiers in pharmacology · 2026Article
- Small Molecule Modulation of MHC-I Surface Expression: A Click Chemistry-Based Discovery Approach.Journal of medicinal chemistry · 2025Article
- The highs and lows of monoamine oxidase as molecular target in cancer: an updated review.Molecular and cellular biochemistry · 2025Review
- Targeting monoamine oxidases in cancer: advances and opportunities.Trends in molecular medicine · 2025Review
- Repurposing of nervous system drugs for cancer treatment: recent advances, challenges, and future perspectives.Discover oncology · 2025Review
- Beyond CTLA-4 and PD-1: Novel Insights into MAO-A as a Next Generation Immune Checkpoint Modulator for Cancer Immunotherapy.Current cancer drug targets · 2025Review
- Heat shock proteins as hallmarks of cancer: insights from molecular mechanisms to therapeutic strategies.Journal of hematology & oncology · 2024Review
Corrections and comments
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Authors and funding
11 authors at 3 institutions in 2 countries.
Funding
Abstract
Monoamine oxidase A (MAO A) and heat shock protein 90 (HSP90) inhibitors have been shown to decrease the progression of glioblastoma (GBM) and other cancers. In this study, a series of MAO A/HSP90 dual inhibitors were designed and synthesized in the hope to develop more effective treatment of GBM. Compounds 4-b and 4-c are conjugates of isopropylresorcinol (pharmacophore of HSP90 inhibitor) with the phenyl group of clorgyline (MAO A inhibitor) by a tertiary amide bond substituted with methyl (4-b) or ethyl (4-c) group, respectively. They inhibited MAO A activity, HSP90 binding, and the growth of both TMZ-sensitive and -resistant GBM cells. Western blots showed that they increased HSP70 expression indicating reduced function of HSP90, reduced HER2 and phospho-Akt expression similar to MAO A or HSP90 inhibitor itself. Both compounds decreased IFN-γ induced PD-L1 expression in GL26 cells, suggesting they can act as immune checkpoint inhibitor. Further, they reduced tumor growth in GL26 mouse model. NCI-60 analysis showed they also inhibited the growth of colon cancer, leukemia, non-small cell lung and other cancers. Taken together, this study demonstrates MAO A/HSP90 dual inhibitors 4-b and 4-c reduced the growth of GBM and other cancers, and they have potential to inhibit tumor immune escape.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.