ArticleBioorganic & medicinal chemistry letters2012
Analogs of the RSK inhibitor SL0101: optimization of in vitro biological stability.
Article in Bioorganic & medicinal chemistry letters, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 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
15 citing papers in PubMed, 31 citations in OpenAlex.
- Carbamate-Bearing Carbohydrates: Natural Occurrence, Pharmacological Relevance, and Chemical Synthesis.ACS omega · 2026Review
- Article
- Therapeutic targeting of p90 ribosomal S6 kinase.Frontiers in cell and developmental biology · 2023Review
- Rhamnose-Containing Compounds: Biosynthesis and Applications.Molecules (Basel, Switzerland) · 2022Review
- Repurposed floxacins targeting RSK4 prevent chemoresistance and metastasis in lung and bladder cancer.Science translational medicine · 2021Article
- RSK Isoforms in Acute Myeloid Leukemia.Biomedicines · 2021Review
- Synthesis, PASS-Predication and in Vitro Antimicrobial Activity of Benzyl 4-O-benzoyl-α-l-rhamnopyranoside Derivatives.International journal of molecular sciences · 2016Article
- Myricetin inhibits proliferation and induces apoptosis and cell cycle arrest in gastric cancer cells.Molecular and cellular biochemistry · 2015Article
- RSK promotes prostate cancer progression in bone through ING3, CKAP2, and PTK6-mediated cell survival.Molecular cancer research : MCR · 2015Article
- Synthesis and Structure-Activity Relationship Study of 5a-Carbasugar Analogues of SL0101.ACS medicinal chemistry letters · 2015Article
- Myricetin exerts anti-proliferative, anti-invasive, and pro-apoptotic effects on esophageal carcinoma EC9706 and KYSE30 cells via RSK2.Tumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine · 2014Article
- De novo synthesis and biological evaluation of C6″-substituted C4″-amide analogues of SL0101.Organic letters · 2014Article
- Astragalus saponins affect proliferation, invasion and apoptosis of gastric cancer BGC-823 cells.Diagnostic pathology · 2013Article
- The Role of Mitogen-Activated Protein Kinase-Activated Protein Kinases (MAPKAPKs) in Inflammation.Genes · 2013Article
- Improving the affinity of SL0101 for RSK using structure-based design.ACS medicinal chemistry letters · 2012Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
The Ser/Thr protein kinase, RSK, is important in the etiology of tumor progression including invasion and motility. The natural product kaempferol-3-O-(3″,4″-di-O-acetyl-α-l-rhamnopyranoside), called SL0101, is a highly specific RSK inhibitor. Acylation of the rhamnose moiety is necessary for high affinity binding and selectivity. However, the acetyl groups can be cleaved by esterases, which accounts for the poor in vitro biological stability of SL0101. To address this problem a series of analogs containing acetyl group replacements were synthesized and their in vitro stability evaluated. Monosubstituted carbamate analogs of SL0101 showed improved in vitro biological stability while maintaining specificity for RSK. These results should facilitate the development of RSK inhibitors derived from SL0101 as anticancer agents.
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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.