Efficient Synthetic Approach to Linear Dasatinib-DNA Conjugates by Click Chemistry.
Bioconjugate chemistry
confidence
Key findings
Synthetic approaches to linear dasatinib-DNA conjugates via click chemistry described; conjugates-derived gold nanoparticles show efficacy against leukemia cells with reduced toxicity.
View source on PubMed (PMID 27690393) ↗
- Sample size
- not reported
- Population
- not applicable (synthetic chemistry study)
- Dosing
- not reported
- Duration
- not reported
- Route
- not reported
- Blinding
- not_reported
- Controls
- active_comparator
- Drug class
- senolytic
Full abstract
A pair of synthetic approaches to linear dasatinib-DNA conjugates via click chemistry are described. The first approach involves the reaction of excess azido dasatinib derivative with 5'-(5-hexynyl)-tagged DNAs, and the second involves the reaction of excess alkynyl-linked dasatinib with 5'-azido-tagged DNA. The second approach using alkynyl-derived dasatinib and 5'-azido-tagged DNA yielded the corresponding dasatinib-DNA conjugates in higher yield (47% versus 10-33% for the first approach). Studies have shown these linear dasatinib-DNA conjugates-derived gold nanoparticles exhibit efficacy against leukemia cancer cells with reduced toxicity toward normal cells compared to that of free dasatinib.