ArticleJournal of medicinal chemistry2014
Design, synthesis, and biological evaluations of tumor-targeting dual-warhead conjugates for a taxoid-camptothecin combination chemotherapy.
Article in Journal of medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
What it found
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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
20 citing papers in PubMed, 71 citations in OpenAlex.
- Article
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- Engineered mesoporous silica nanosystems with organotin(IV) complexes containing 1-(quinolin-8-yliminomethyl)naphthalen-2-ol ligand for cancer cell targeting.Dalton transactions (Cambridge, England : 2003) · 2025Article
- A Water-Soluble Small Molecule Boron Carrier Targeting Biotin Receptors for Neutron Capture Therapy.ACS omega · 2024Article
- Facile Synthesis of FimH Antagonist and Its Analogues: Simple Entry to ComplexACS medicinal chemistry letters · 2024Article
- Strategies for the drug discovery and development of taxane anticancer therapeutics.Expert opinion on drug discovery · 2022Review
- Porphyrin-Based Tumor-Targeting Theranostic Agent: Gd-TDAP.ACS medicinal chemistry letters · 2021Article
- Discovery of potent nucleotide pyrophosphatase/phosphodiesterase3 (NPP3) inhibitors with ancillary carbonic anhydrase inhibition for cancer (immuno)therapy.RSC medicinal chemistry · 2021Article
- Multifunctional Neomycin-Triazine-Based Cationic Lipids for Gene Delivery with Antibacterial Properties.Bioconjugate chemistry · 2021Article
- Single- versus Dual-Targeted Nanoparticles with Folic Acid and Biotin for Anticancer Drug Delivery.Pharmaceutics · 2021Review
- Nanoparticle-Based Delivery of CRISPR/Cas9 Genome-Editing Therapeutics.The AAPS journal · 2018Review
- 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
- [Targeted imaging ability of a biotinylated imaging probe Biotin-S-S-Rhodol for breast cancer cells in vitro].Nan fang yi ke da xue xue bao = Journal of Southern Medical University · 2017Article
- A nanoparticulate pre-chemosensitizer for efficacious chemotherapy of multidrug resistant breast cancer.Scientific reports · 2016Article
- Protecting the normal in order to better kill the cancer.Cancer medicine · 2015Review
- Design, synthesis, and biological evaluation of theranostic vitamin-linker-taxoid conjugates.Journal of medicinal chemistry · 2015Article
- Design, Synthesis and Application of Fluorine-Labeled Taxoids asJournal of fluorine chemistry · 2015Article
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
Novel tumor-targeting dual-warhead conjugates, 2 (DW-1) and 3 (DW-2), which consist of a next-generation taxoid, 1 (SB-T-1214), and camptothecin as two warheads, self-immolative disulfide linkers for drug release, biotin as the tumor-targeting moiety, and 1,3,5-triazine as the tripod splitter module, were designed and synthesized. The potency of 2 was evaluated against MX-1, MCF-7, ID8, L1210FR (BR+, biotin receptor overexpressed) and WI38 (BR-, normal) cell lines in the absence and presence of glutathione (GSH), which is an endogenous thiol that triggers drug release inside the cancer cells. With the GSH and resuspension protocol, 2 exhibited IC50 values of 3.22-9.80 nM against all BR+ cancer cell lines, and 705 nM against WI38. Thus, there was a two orders of magnitude higher selectivity to cancer cells. Also, a clear cooperative effect was observed for the taxoid-camptothecin combination when two drugs were delivered to the cancer cells specifically in the form of a dual-warhead conjugate.
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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.