ArticleACS medicinal chemistry letters2015
Design, synthesis, and biological evaluation of ring-constrained novobiocin analogues as hsp90 C-terminal inhibitors.
Article in ACS medicinal chemistry letters, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
17 citing papers in PubMed, 33 citations in OpenAlex.
- Evolution of Hsp90 targeting: From stress biology to clinical translation.Cell stress & chaperones · 2026Review
- The evolution of heat shock protein 90 C-terminal inhibitors: From novobiocin to potential clinical candidates.Cell stress & chaperones · 2026Review
- Sugar mimics and their probable binding sites: design and synthesis of thiazole linked coumarin-piperazine hybrids as galectin-1 inhibitors.RSC advances · 2024Article
- Heterocyclic Compounds as Hsp90 Inhibitors: A Perspective on Anticancer Applications.Pharmaceutics · 2022Review
- The quest for supernatural products: the impact of total synthesis in complex natural products medicinal chemistry.Natural product reports · 2020Review
- Heat shock protein 90 inhibition and multi-target approach to maximize cardioprotection in ischaemic injury.British journal of pharmacology · 2020Review
- New N-phenylpyrrolamide DNA gyrase B inhibitors: Optimization of efficacy and antibacterial activity.European journal of medicinal chemistry · 2018Article
- Synthesis of Novel Amino Acid-Fipronil Conjugates and Study on Their Phloem Loading Mechanism.Molecules (Basel, Switzerland) · 2018Article
- Discovery of new molecular entities able to strongly interfere with Hsp90 C-terminal domain.Scientific reports · 2018Article
- Development of noviomimetics that modulate molecular chaperones and manifest neuroprotective effects.European journal of medicinal chemistry · 2018Article
- Synthesis and Biological Evaluation of Stilbene Analogues as Hsp90 C-Terminal Inhibitors.ChemMedChem · 2017Article
- Development of Phenyl Cyclohexylcarboxamides as a Novel Class of Hsp90 C-terminal Inhibitors.Chemistry (Weinheim an der Bergstrasse, Germany) · 2017Article
- Design, synthesis and biological evaluation of alkylamino biphenylamides as Hsp90 C-terminal inhibitors.Bioorganic & medicinal chemistry · 2017Article
- Diverging Novobiocin Anti-Cancer Activity from Neuroprotective Activity through Modification of the Amide Tail.ACS medicinal chemistry letters · 2016Article
- Synthesis and Biological Evaluation of Novobiocin Core Analogues as Hsp90 Inhibitors.Chemistry (Weinheim an der Bergstrasse, Germany) · 2016Article
- Transportable, Chemical Genetic Methodology for the Small Molecule-Mediated Inhibition of Heat Shock Factor 1.ACS chemical biology · 2016Article
- Anticancer Inhibitors of Hsp90 Function: Beyond the Usual Suspects.Advances in cancer research · 2016Review
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Hsp90 C-terminal inhibitors represent a novel and alternative chemotherapeutic approach for the treatment of cancer. Novobiocin was the first natural product identified as an Hsp90 C-terminal inhibitor; however, it manifests poor antiproliferative activity. In contrast to N-terminal inhibitors, novobiocin does not induce the pro-survival heat shock response. Structural investigations on novobiocin have elucidated some structure-activity relationships and several promising compounds. On the basis of structure-activity relationships and computational studies, a library of ring-constrained novobiocin analogues was designed, synthesized, and evaluated in antiproliferative assays. Results obtained from these studies provide insights into the Hsp90 C-terminal binding site, and new analogues that were developed manifest low micromolar to mid-nanomolar antiproliferative activity resulting from Hsp90 inhibition.
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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.