ArticleBioorganic & medicinal chemistry letters2016
Derivatization of agelastatin A leading to bioactive analogs and a trifunctional probe.
Article in Bioorganic & medicinal chemistry letters, 2016. 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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Who cites it
9 citing papers in PubMed.
- Proteome-Wide Profiling of Olaparib Interactors Using a Biotinylated Photoaffinity Probe.Chembiochem : a European journal of chemical biology · 2025Article
- Exploring Marine Alkaloids: A Natural Approach to Cancer Treatment.Current pharmaceutical biotechnology · 2025Review
- Ribosomal rodeo: wrangling translational machinery in gynecologic tumors.Cancer metastasis reviews · 2024Review
- The Interplay Between theInternational journal of molecular sciences · 2024Review
- TheMolecules (Basel, Switzerland) · 2023Article
- Synthesis of Agelastatin A and Derivatives Premised on a Hidden Symmetry Element Leading to Analogs Displaying Anticancer Activity.Tetrahedron · 2021Article
- Olaparib-Based Photoaffinity Probes for PARP-1 Detection in Living Cells.Chembiochem : a European journal of chemical biology · 2020Article
- Synthesis and Evaluation of Agelastatin Derivatives as Potent Modulators for Cancer Invasion and Metastasis.The Journal of organic chemistry · 2017Article
- Inhibition of Eukaryotic Translation by the Antitumor Natural Product Agelastatin A.Cell chemical biology · 2017Article
Corrections and comments
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Authors and funding
11 authors.
Funding
Abstract
(-)-Agelastatin A (AglA, 1), a member of the pyrrole-aminoimidazole marine alkaloid (PAI) family, possesses a unique tetracyclic structure and is one of the most potent anticancer PAIs isolated to date. In efforts to expand the SAR of these agents and delineate sites that tolerate modification while retaining activity, we synthesized several derivatives and tested their anticancer activity. The cytotoxic effects of these derivatives were measured against several cancer cell lines including cervical cancer (HeLa), epidermoid carcinoma (A431), ovarian (Igrov and Ovcar3), osteosarcoma (SJSA1), acute T cell leukemia (A3), epidermoid carcinoma (A431) in addition to primary human chronic lymphocytic leukemia (CLL) cells. New positions for modification of AglA and new substitutions were explored leading to novel derivatives, 14-chloro AglA (3) and 14-methyl AglA (12), that retained activity toward various cancer cell lines with decreased toxicity toward B- and T-cells. The SAR data informed the synthesis of a trifunctional probe bearing an alkyne and a diazirine potentially useful for cellular target identification.
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Registered trials
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