ArticleAngewandte Chemie (International ed. in English)2020
Expeditious Total Synthesis of Hemiasterlin through a Convergent Multicomponent Strategy and Its Use in Targeted Cancer Therapeutics.
Article in Angewandte Chemie (International ed. in English), 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed, 19 citations in OpenAlex.
- Targeting Folate Receptors for the Detection and Selective Treatment of Cancer: Advanced Precision Oncology in Practice.International journal of biological sciences · 2026Review
- Multicomponent Synthesis of the SARS-CoV-2 Main Protease Inhibitor Nirmatrelvir.The Journal of organic chemistry · 2023Article
- All-in-one disulfide bridging enables the generation of antibody conjugates with modular cargo loading.Chemical science · 2022Article
- Divinylpyrimidine reagents generate antibody-drug conjugates with excellentChemical communications (Cambridge, England) · 2022Article
- Antibody-Antineoplastic Conjugates in Gynecological Malignancies: Current Status and Future Perspectives.Pharmaceutics · 2021Review
- Rapid and robust cysteine bioconjugation with vinylheteroarenes.Chemical science · 2021Article
- Expeditious Total Synthesis of Hemiasterlin through a Convergent Multicomponent Strategy and Its Use in Targeted Cancer Therapeutics.Angewandte Chemie (International ed. in English) · 2020Article
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
Hemiasterlin is an antimitotic marine natural product with reported sub-nanomolar potency against several cancer cell lines. Herein, we describe an expeditious total synthesis of hemiasterlin featuring a four-component Ugi reaction (Ugi-4CR) as the key step. The convergent synthetic strategy enabled rapid access to taltobulin (HTI-286), a similarly potent synthetic analogue. This short synthetic sequence enabled investigation of both hemiasterlin and taltobulin as cytotoxic payloads in antibody-drug conjugates (ADCs). These novel ADCs displayed sub-nanomolar cytotoxicity against HER2-expressing cancer cells, while showing no activity against antigen-negative cells. This study demonstrates an improved synthetic route to a highly valuable natural product, facilitating further investigation of hemiasterlin and its analogues as potential payloads in targeted therapeutics.
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Registered trials
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