Synthesis and Antiproliferative Effect of New Alkyne-Tethered Vindoline Hybrids Containing Pharmacophoric Fragments
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...
Elmentve itt :
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| Dokumentumtípus: | Cikk |
| Megjelent: |
2024
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| Sorozat: | INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
25 No. 13 |
| doi: | 10.3390/ijms25137428 |
| mtmt: | 35087983 |
| Online Access: | http://publicatio.bibl.u-szeged.hu/39770 |
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| 024 | 7 | |a 35087983 |2 mtmt | |
| 040 | |a SZTE Publicatio Repozitórium |b hun | ||
| 041 | |a eng | ||
| 100 | 1 | |a Ferenczi Etelka | |
| 245 | 1 | 0 | |a Synthesis and Antiproliferative Effect of New Alkyne-Tethered Vindoline Hybrids Containing Pharmacophoric Fragments |h [elektronikus dokumentum] / |c Ferenczi Etelka |
| 260 | |c 2024 | ||
| 300 | |a 20 | ||
| 490 | 0 | |a INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES |v 25 No. 13 | |
| 520 | 3 | |a 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 human embryonal lung fibroblast MRC-5 served as 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. These results suggest that ovarian cancer might be considered as a prioritized target of treatment with 36. | |
| 700 | 0 | 1 | |a Keglevich Péter |e aut |
| 700 | 0 | 1 | |a Tayeb Bizhar Ahmed |e aut |
| 700 | 0 | 1 | |a Minorics Renáta |e aut |
| 700 | 0 | 1 | |a Papp Dávid |e aut |
| 700 | 0 | 1 | |a Schlosser Gitta |e aut |
| 700 | 0 | 1 | |a Zupkó István |e aut |
| 700 | 0 | 1 | |a Hazai László |e aut |
| 700 | 0 | 1 | |a Csámpai Antal |e aut |
| 856 | 4 | 0 | |u http://publicatio.bibl.u-szeged.hu/39770/1/ijms_2024_vindoline_ferenczi_et_al.pdf |z Dokumentum-elérés |