ArticleBioorganic & medicinal chemistry2010
Design and synthesis of Hsp90 inhibitors: exploring the SAR of Sansalvamide A derivatives.
Article in Bioorganic & medicinal chemistry, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 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
28 citing papers in PubMed.
- Heat Shock Protein 90: From Molecular Chaperone Function to Therapeutic Targeting in Malignancies.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Review
- Targeting HSP90 in cancer: advances in the development of inhibitors, mechanisms of action, and therapeutic applications.Molecular cancer · 2026Review
- Anti-cancer properties of Sansalvamide A, its derivatives, and analogs: an updated review.Naunyn-Schmiedeberg's archives of pharmacology · 2024Review
- Influence of heterochirality on the structure, dynamics, biological properties of cyclic(PFPF) tetrapeptides obtained by solvent-free ball mill mechanosynthesis.Scientific reports · 2024Article
- Development of a First-in-Class Small-Molecule Inhibitor of the C-Terminal Hsp90 Dimerization.ACS central science · 2022Article
- Head-to-tail cyclization of side chain-protected linear peptides to recapitulate genetically-encoded cyclized peptides.Peptide science (Hoboken, N.J.) · 2022Article
- Article
- Delivering bioactive cyclic peptides that target Hsp90 as prodrugs.Journal of enzyme inhibition and medicinal chemistry · 2019Article
- Article
- PET imaging of Hsp90 expression in pancreatic cancer using a newAmino acids · 2018Article
- Biscogniauxone, a New Isopyrrolonaphthoquinone Compound from the Fungus Biscogniauxia mediterranea Isolated from Deep-Sea Sediments.Marine drugs · 2016Article
- Anticancer Inhibitors of Hsp90 Function: Beyond the Usual Suspects.Advances in cancer research · 2016Review
- First Structural View of a Peptide Interacting with the Nucleotide Binding Domain of Heat Shock Protein 90.Scientific reports · 2015Article
- The Chemical Biology of Molecular Chaperones--Implications for Modulation of Proteostasis.Journal of molecular biology · 2015Review
- Potential C-terminal-domain inhibitors of heat shock protein 90 derived from a C-terminal peptide helix.Bioorganic & medicinal chemistry · 2014Article
- Chemically accessible hsp90 inhibitor that does not induce a heat shock response.ACS medicinal chemistry letters · 2014Article
- Article
- A heat shock protein 90 inhibitor that modulates the immunophilins and regulates hormone receptors without inducing the heat shock response.Bioorganic & medicinal chemistry letters · 2014Article
- Consecutive isocyanide-based multicomponent reactions: synthesis of cyclic pentadepsipeptoids.Beilstein journal of organic chemistry · 2014Article
- Effectively delivering a unique hsp90 inhibitor using star polymers.ACS medicinal chemistry letters · 2013Article
Corrections and comments
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Authors and funding
16 authors.
Funding
Abstract
Utilizing the structure-activity relationship we have developed during the synthesis of the first two generations and mechanism of action studies that point to the interaction of these molecules with the key oncogenic protein Hsp90, we report here the design of 32 new Sansalvamide A derivatives and their synthesis. Our new structures, designed from previously reported potent compounds, were tested for cytotoxicity on the HCT116 colon cancer cell line, and their binding to the biological target was analyzed using computational studies involving blind docking of derivatives using Autodock. Further, we show new evidence that our molecules bind directly to Hsp90 and modulate Hsp90's binding with client proteins. Finally, we demonstrate that we have integrated good ADME properties into a new derivative.
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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.