ArticleBioorganic & medicinal chemistry2015
Design, synthesis and biological evaluation of a highly-potent and cancer cell selective folate-taxoid conjugate.
Article in Bioorganic & medicinal chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 33 citations in OpenAlex.
- Article
- Molecular impact of NOTCH signaling dysregulation on ovarian cancer progression, chemoresistance, and taxane response.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie · 2025Article
- Folate-engineered chitosan nanoparticles: next-generation anticancer nanocarriers.Molecular cancer · 2024Review
- Third-generation taxanes SB-T-121605 and SB-T-121606 are effective in pancreatic ductal adenocarcinoma.iScience · 2024Article
- Development of PROTACS degrading KRAS and SOS1.Oncology research · 2024Review
- Strategies for the drug discovery and development of taxane anticancer therapeutics.Expert opinion on drug discovery · 2022Review
- Effect of Trimethine Cyanine Dye- and Folate-Conjugation on the In Vitro Biological Activity of Proapoptotic Peptides.Biomolecules · 2022Article
- Anticancer regimens containing third generation taxanes SB-T-121605 and SB-T-121606 are highly effective in resistant ovarian carcinoma model.Frontiers in pharmacology · 2022Article
- Active Targeted Nanoformulations via Folate Receptors: State of the Art and Future Perspectives.Pharmaceutics · 2021Review
- Cellular delivery of dinucleotides by conjugation with small molecules: targeting translation initiation for anticancer applications.Chemical science · 2021Article
- A step-wise synthetic approach is necessary to access γ-conjugates of folate: folate-conjugated prodigiosenes.RSC advances · 2019Article
- Design, Synthesis, and Biological Evaluations of Asymmetric Bow-Tie PAMAM Dendrimer-Based Conjugates for Tumor-Targeted Drug Delivery.ACS omega · 2018Article
- Quest for Efficacious Next-Generation Taxoid Anticancer Agents and Their Tumor-Targeted Delivery.Journal of natural products · 2018Review
- Advances in targeting the folate receptor in the treatment/imaging of cancers.Chemical science · 2018Review
- Strategic Incorporation of Fluorine into Taxoid Anticancer Agents for Medicinal Chemistry and Chemical Biology Studies.Journal of fluorine chemistry · 2017Article
- Taxane anticancer agents: a patent perspective.Expert opinion on therapeutic patents · 2016Review
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
The folate receptor (FR) has been widely recognized as an excellent target for the tumor-selective delivery of cytotoxic agents, and four folate-drug conjugates have entered clinical evaluations for the treatment of solid tumors to date. However, most of these conjugates required structural modification of the cytotoxic warheads in order to achieve efficient drug release from the linkers. We designed and constructed a novel folate conjugate of a highly-potent next-generation taxoid, SB-T-1214, by exploiting bioorthogonal Cu-free 'click' chemistry. The synthesis was highly convergent and required no HPLC purification to obtain the final folate-taxoid conjugate 1. Conjugate 1 demonstrated highly FR-specific potency (IC₅₀ 2.1-3.5 nM) against a panel of cancer cell lines, with a >1000-fold decrease in cytotoxicity against normal human cells (IC₅₀>5000 nM). The remarkable potency and selectivity of conjugate 1 can be attributed to highly FR-specific receptor-mediated endocytosis as well as efficient release of the unmodified cytotoxic warhead using a mechanism-based self-immolative linker.
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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.