ArticleChemMedChem2025
Exploration of the Tertiary Amide Chemical Space of Dolastatin 15 Analogs Reveals New Insights into the Structure-Anticancer Activity Relationship.
Article in ChemMedChem, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.
What it found
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Who cites it
5 citing papers in PubMed.
- Synthesis and Evaluation of Peptoid-Based Compound Libraries as Inhibitors of Parasite Metallo-Aminopeptidases.ChemMedChem · 2026Article
- Marine Bioactive Peptides for Colorectal Cancer Therapy: Mechanisms, Therapeutic Potential, and Translational Challenges.Marine drugs · 2026Review
- Impact of C-Terminal AmideMolecules (Basel, Switzerland) · 2026Article
- Synthetic Linear Lipopeptides and Lipopeptoids Induce Apoptosis and Oxidative Stress: In Vitro Cytotoxicity and SAR Evaluation Against Cancer Cell Lines.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Exploration of the Tertiary Amide Chemical Space of Dolastatin 15 Analogs Reveals New Insights into the Structure-Anticancer Activity Relationship.ChemMedChem · 2025Article
Corrections and comments
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Authors and funding
10 authors.
Funding
Abstract
Dolastatins are a class of naturally occurring antimitotic peptides that have inspired the development of some of the most active and widely used anticancer agents. Here, we report on the development of synthetic methodologies for the preparation of parallel libraries of small peptides inspired by dolastatin 15 and its analogs cemadotin and tasidotin. The approaches rely on the use of either one or multiple Ugi-multicomponent reactions to generate amide N-substituted dolastatin-like skeletons, which allow the exploration of tertiary amide chemical spaces that have not been assessed previously. Evaluation of the anticancer activity in a variety of cancer cells showed that introducing a tertiary amide at the C-terminal fragment or by replacement of a proline residue does not lead to an increment in the anti-proliferative activity. The microtubule-disrupting capacity of the new dolastatin analogs was studied and compared with other potent antimitotic agents, thereby shedding light on mechanistic details of their anti-proliferative activity.
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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.