Rational design of thiazolidine-2,4-dione-integrated combretastatin A-4 analogues as potent and selective tubulin-targeting agents for triple-negative breast cancer
Yazarlar (1)
Doç. Dr. Feyzi Sinan TOKALI Kafkas Üniversitesi, Türkiye
| Makale Türü | Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale) | ||
| Dergi Adı | European Journal of Medicinal Chemistry (Q1) | ||
| Dergi ISSN | 0223-5234 Dergi Bilgileri (2026) | ||
| Dergi Tarandığı Indeksler | SCI-Expanded | ||
| Makale Dili | İngilizce | Basım Tarihi | 12-2026 |
| Kabul Tarihi | 20-08-2026 | Yayınlanma Tarihi | 24-08-2026 |
| Cilt / Sayı / Sayfa | 319 / 1 / – | DOI | 10.1016/j.ejmech.2026.119270 |
| Makale Linki | https://doi.org/10.1016/j.ejmech.2026.119270 | ||
| UAK Araştırma Alanları |
Organik Kimya
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| Özet |
| Microtubule-targeting agents remain among the most effective chemotherapeutics for the treatment of cancer. Inspired by the natural tubulin polymerization inhibitor combretastatin A-4 (CA-4), a series of novel thiazolidine-2,4-dione derivatives was designed, synthesized, and evaluated as potential tubulin-targeting anticancer agents. The cytotoxic activities of the compounds were assessed against the MDA-MB-231, while human umbilical vein endothelial cells (HUVEC) were employed to evaluate selectivity. Compounds 2 and 3 emerged as the most active members of the series (IC 50 = 3.60 and 3.71 μM, respectively), accompanied by remarkably high selectivity indices of 49.7 and 51.3. To elucidate their mechanism of action, compounds 2 and 3 were further evaluated in an in vitro tubulin polymerization assay. Compound 3 displayed the strongest inhibitory activity (IC 50 = 1.07 μM), surpassing the ... |
| Anahtar Kelimeler |
| Breast cancer | Combretastatin A-4 | Inhibition | Thiazolidine-2,4-dione | Tubulin polymerization |
Science Direct
Rational design of thiazolidine-2,4-dione-integrated combretastatin A-4 analogues as potent and selective tubulin-targeting agents for triple-negative breast cancer
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| Google Scholar | 1 |