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- Title
Synthesis and Antiproliferative Effect of New Alkyne-Tethered Vindoline Hybrids Containing Pharmacophoric Fragments.
- Authors
Ferenczi, Etelka; Keglevich, Péter; Tayeb, Bizhar Ahmed; Minorics, Renáta; Papp, Dávid; Schlosser, Gitta; Zupkó, István; Hazai, László; Csámpai, Antal
- Abstract
In the frame of our diversity-oriented research on multitarget small molecule anticancer agents, utilizing convergent synthetic sequences terminated by Sonogashira coupling reactions, a preliminary selection of representative alkyne-tethered vindoline hybrids was synthesized. The novel hybrids with additional pharmacophoric fragments of well-documented anticancer agents, including FDA-approved tyrosine-kinase inhibitors (imatinib and erlotinib) or ferrocene or chalcone units, were evaluated for their antiproliferative activity on malignant cell lines MDA-MB-231 (triple negative breast cancer), A2780 (ovarian cancer), HeLa (human cervical cancer), and SH-SY5Y (neuroblastoma) as well as on human embryonal lung fibroblast cell line MRC-5, which served as a reference non-malignant cell line for the assessment of the therapeutic window of the tested hybrids. The biological assays identified a trimethoxyphenyl-containing chalcone-vindoline hybrid (36) as a promising lead compound exhibiting submicromolar activity on A2780 cells with a marked therapeutic window.
- Subjects
UNITED States. Food &; Drug Administration; ERLOTINIB; CHALCONE; TRIPLE-negative breast cancer; COUPLING reactions (Chemistry); PROTEIN-tyrosine kinase inhibitors; BIOLOGICAL assay; SONOGASHIRA reaction
- Publication
International Journal of Molecular Sciences, 2024, Vol 25, Issue 13, p7428
- ISSN
1661-6596
- Publication type
Article
- DOI
10.3390/ijms25137428