ArticleTetrahedron2011
Function Oriented Synthesis: Preparation and Initial Biological Evaluation of New A-Ring-Modified Bryologs.
Article in Tetrahedron, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
What it found
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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.
The trial behind it
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
4 citing papers in PubMed.
- Capturing Biological Activity in Natural Product Fragments by Chemical Synthesis.Angewandte Chemie (International ed. in English) · 2016Review
- Improved protein kinase C affinity through final step diversification of a simplified salicylate-derived bryostatin analog scaffold.Organic letters · 2014Article
- Synthesis of seco-B-ring bryostatin analogue WN-1 via C-C bond-forming hydrogenation: critical contribution of the B-ring in determining bryostatin-like and phorbol 12-myristate 13-acetate-like properties.Journal of the American Chemical Society · 2014Article
- Microbial natural products: molecular blueprints for antitumor drugs.Journal of industrial microbiology & biotechnology · 2013Review
Corrections and comments
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Authors and funding
2 authors.
Funding
Abstract
The synthesis and biological evaluation of the first members of a new series of designed bryostatin A-ring analogues (bryologs) are described. An advanced intermediate is produced that allows for step economical access to diverse analogs. The first of these analogues, bearing side chains of completely different polarities from alkyl to hydroxyl and carboxyl functionalities, were evaluated. All exhibit potent protein kinase C binding (54.7 to 2.4 nM) with affinities increasing with decreasing side chain polarity. This series of bryostatin analogues demonstrates that A ring surrogates can indeed be used for tuning pharmacophore and ADME characteristics as needed to improve bryolog function.
Identifiers
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Registered trials
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