Highly promising antitumor agent of a novel Platinum(II) complex bearing a tetradentate chelating ligand
Yükleniyor...
Dosyalar
Tarih
2020
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
Amer Chemical Soc
Erişim Hakkı
info:eu-repo/semantics/openAccess
Özet
A new mononuclear cationic platinum(II) coordination compound with 6,6'-bis(NH-benzimidazol-2-yl)-2,2'-bipyridine (L) ligand having N-4-tetradentate binding pocket [Pt(L)]-Cl-2.2H(2)O (Complex 1) was synthesized and characterized by FTIR(ATR), UV-vis, H-1 NMR, APCI and MALDI MS, and CHN analysis. The antigrowth effect of Complex 1 was tested in breast cancer (MDA-MB-231), lung cancer (A549), colorectal cancer (HCT-116), prostate cancer (PC-3) cell lines, and bronchial epithelial cell line (BEAS-2B) by the SRB and ATP cell viability assays. Apoptosis was detected with Annexin V, mitopotential, BCL-2 inactivation, and gamma H2AX assays by flow cytometry. Complex 1 was found to have cytotoxic activity of MDA-MB-231, A549, HCT-116, and PC-3 cancer cell lines in a dose-dependent manner for 48 h. Complex 1 has been found to cause cell death through different mechanisms depending on the type of cancer. The findings indicated that complex induced intrinsic apoptosis with the increased mitochondrial membrane depolarization level, Bcl-2 inactivation, and DNA damage in PC-3 and A549 cell lines.
Açıklama
YILMAZ, ismail/0000-0002-0139-0122; Erkisa, Merve/0000-0002-3127-742X; Ulukaya, Engin/0000-0003-4875-5472; AKAR, Okan/0000-0001-8687-2034
Akar, Okan Remzi ; Erkisa Genel, Merve ; Selvi, Selin ; Ulukaya, Engin (isu author)
Akar, Okan Remzi ; Erkisa Genel, Merve ; Selvi, Selin ; Ulukaya, Engin (isu author)
Anahtar Kelimeler
Platinum, N-4-Donor Ligand, Benzimidazole, Pyridine, Cytotoxicity, Apoptosis
Kaynak
Acs Medicinal Chemistry Letters
WoS Q Değeri
Q2
Scopus Q Değeri
Q1
Cilt
11
Sayı
5
Künye
Yilmaz, I., Akar, O. R., Erkisa, M., Selvi, S., Sengul, A., & Ulukaya, E. (2020). Highly Promising Antitumor Agent of a Novel Platinum(II) Complex Bearing a Tetradentate Chelating Ligand. ACS MEDICINAL CHEMISTRY LETTERS, 11(5), 940–948. https://doi.org/10.1021/acsmedchemlett.9b00676
