ArticleJournal of medicinal chemistry2011
Synthesis and biological evaluation of analogues of AKT (protein kinase B) inhibitor-IV.
Article in Journal of medicinal chemistry, 2011. 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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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
9 citing papers in PubMed, 77 citations in OpenAlex.
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- Insights into the Formations of Host-Guest Complexes Based on the Benzimidazolium Based Ionic Liquids-β-Cyclodextrin Systems.ACS physical chemistry Au · 2022Article
- Benzothiazoles as potential antiviral agents.The Journal of pharmacy and pharmacology · 2020Review
- Discovery of Antibacterials That Inhibit Bacterial RNA Polymerase Interactions with Sigma Factors.Journal of medicinal chemistry · 2020Article
- Article
- Anticancer/antiviral agent Akt inhibitor-IV massively accumulates in mitochondria and potently disrupts cellular bioenergetics.ACS chemical biology · 2015Article
- Recent syntheses of PI3K/Akt/mTOR signaling pathway inhibitors.Bioorganic & medicinal chemistry · 2013Review
- Modulation of the Akt pathway reveals a novel link with PERK/eIF2α, which is relevant during hypoxia.PloS one · 2013Article
- Pd(II)-catalyzed ortho arylation of 2-arylbenzothiazoles with aryl iodides via benzothiazole-directed C-H activation.Journal of organometallic chemistry · 2012Article
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 1 country.
Funding
Abstract
Inhibitors of the PI3-kinase/AKT (protein kinase B) pathway are under investigation as anticancer and antiviral agents. The benzimidazole derivative AKT inhibitor-IV (ChemBridge 5233705) affects this pathway and exhibits potent anticancer and antiviral activity. To probe its biological activity, we synthesized AKT inhibitor-IV and 21 analogues using a novel six-step route based on ZrCl(4)-catalyzed cyclization of 1,2-arylenediamines with α,β-unsaturated aldehydes. We examined effects on viability of HeLa carcinoma cells, viability of normal human cells (NHBE), replication of recombinant parainfluenza virus 5 (PIV5) in HeLa cells, and replication of the intracellular bacterium Mycobacterium fortuitum in HeLa cells. Replacement of the benzimidazole N-ethyl substitutent of AKT inhibitor-IV with N-hexyl and N-dodecyl groups enhanced antiviral activity and cytotoxicity against the cancer cell line, but these compounds showed substantially lower toxicity (from 6-fold to >20-fold) against NHBE cells and no effect on M. fortuitum, suggesting inhibition of one or more host protein(s) required for proliferation of cancer cells and PIV5. The key structural elements identified here may facilitate identification of targets of this highly biologically active scaffold.
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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 OpenQuestion graph.