FETPY: a Diiron(I) Thio–Carbyne Complex with Prominent Anticancer Activity In Vitro and In Vivo
2024
Аутори:
Mihajlović, EkatarinaBiancalana, Lorenzo
Jelača, Sanja
Chiaverini, Lorenzo
Dojčinović, Biljana
Dunđerović, Duško
Zacchini, Stefano
Mijatović, Sanja
Maksimović-Ivanić, Danijela
Marchetti, Fabio
Тип документа:
Чланак у часопису (Објављена верзија)
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© 2024 American Chemical Society
Метаподаци
Приказ свих података о документуАпстракт:
FETPY, an organo-diiron(I) complex, showed strong cytotoxicity across a panel of human and mouse cancer cell lines, combined with an outstanding selectivity compared to nonmalignant cells. Enhanced iron uptake in aggressive, low-differentiated cell lines, caused membrane lipid peroxidation, which resulted in ferroptosis in human ovarian cancer cells. FETPY induced significant morphological changes in murine B16–F1 and B16–F10 melanoma cells, leading to senescence and/or trans-differentiation into Schwann-like cells, thus significantly reducing their tumorigenic potential. Additionally, FETPY substantially suppressed tumor growth in low- and high-grade syngeneic melanoma models when administered in a therapeutic regimen. FETPY is featured by satisfactory water solubility (millimolar range), an amphiphilic character (Log Pow = −0.17), and excellent stability in a biological medium (DMEM). These important requisites for drug development are rarely met in iron complexes investigated so far as possible anticancer agents. Overall, FETPY holds promise as a safe and potent targeted antitumor agent.
Извор:
Journal of Medicinal Chemistry, 2024, 67, 9, 7553-7568Финансирање / пројекти:
- Министарство науке, технолошког развоја и иновација Републике Србије, институционално финансирање - 200007 (Универзитет у Београду, Институт за биолошка истраживања 'Синиша Станковић') (RS-MESTD-inst-2020-200007)
- Fondi di Ateneo 2020
DOI: 10.1021/acs.jmedchem.4c00377
ISSN: 0022-2623
PubMed: 38639401