Scopus
YÖKSİS Eşleşti
Novel mitochondrial and DNA damaging fluorescent Calix[4]arenes bearing isatin groups as aromatase inhibitors: Design, synthesis and anticancer activity
Bioorganic and Medicinal Chemistry · Ocak 2024
YÖKSİS Kayıtları
Novel mitochondrial and DNA damaging fluorescent Calix[4]arenes bearing isatin groups as aromatase inhibitors: Design, synthesis and anticancer activity
Elsevier BV · 2024 SCI-Expanded
PROFESÖR BAHADIR ÖZTÜRK →
Novel mitochondrial and DNA damaging fluorescent Calix[4]arenes bearing isatin groups as aromatase inhibitors: Design, synthesis and anticancer activity
Bioorganic & Medicinal Chemistry · 2024 SCI-Expanded
PROFESÖR MUSTAFA YILMAZ →
Novel mitochondrial and DNA damaging fluorescent Calix[4]arenes bearing isatin groups as aromatase inhibitors: Design, synthesis and anticancer activity
Bioorganic & Medicinal Chemistry · 2024 SCI-Expanded
DOÇENT MEHMET OĞUZ →
Makale Bilgileri
DergiBioorganic and Medicinal Chemistry
Yayın TarihiOcak 2024
Cilt / Sayfa98
Scopus ID2-s2.0-85181569704
Özet
Breast cancer causes a high rate of mortality all over the world. Therefore, the present study focuses on the anticancer activity of new lower rim-functionalized calix[4]arenes integrated with isatin and the p-position of calixarenes with 1,4-dimethylpyridinium iodine against various human cancer cells such as MCF-7 and MDA-MB-231 breast cancer cell lines, as well as the PNT1A healthy epithelial cell line. It was observed that compound 6c had the lowest values in MCF-7 (8.83 µM) and MDA-MB-231 (3.32 µM). Cell imaging and apoptotic activity studies were performed using confocal microscopy and flow cytometry, respectively. The confocal imaging studies with 6c showed that the compound easily entered the cell, and it was observed that 6c accumulated in the mitochondria. The Comet assay test was used to detect DNA damage of compounds in cells. It was found that treated cells had abnormal tail nuclei and damaged DNA structures compared with untreated cells. In vitro human aromatase enzyme inhibition profiles showed that compound 6c had a remarkable inhibitory effect on aromatase. Compound 6c displayed a significant inhibition capacity on aromatase enzyme with the IC50 value of 0.104 ± 0.004 µM. Thus, not only the anticancer activity of the new fluorescent derivatives, which are the subject of this study, but the aromatase inhibitory profiles have also been proven.
Yazarlar (5)
1
Alev Oguz
2
Begum Nurpelin Saglik
3
Mehmet Oguz
4
Bahadır Öztürk
5
Mustafa Yilmaz
Anahtar Kelimeler
Anticancer
Aromatase inhibition
Calixarene
Cell imaging
Isatin
Kurumlar
Anadolu Üniversitesi
Eskisehir Turkey
Selçuk Üniversitesi
Selçuklu Turkey
Metrikler
1
Atıf
5
Yazar
5
Anahtar Kelime