Synthesis and characterisation of novel tricyclic and tetracyclic furoindoles: Biological evaluation as SAHA enhancer against neuroblastoma and breast cancer cells
Yükleniyor...
Tarih
2021
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
MDPI
Erişim Hakkı
info:eu-repo/semantics/openAccess
Özet
The dihydropyranoindole structures were previously identified as promising scaffolds for improving the anti-cancer activity of histone deacetylase inhibitors. This work describes the synthesis of related furoindoles and their ability to synergize with suberoylanilide hydroxamic acid (SAHA) against neuroblastoma and breast cancer cells. The nucleophilic substitution of hydroxyin-dole methyl esters with α-haloketones yielded the corresponding arylether ketones, which were subsequently cyclized to tricyclic and tetracyclic furoindoles. The furoindoles showed promising individual cytotoxic efficiency against breast cancer cells, as well as decent SAHA enhancement against cancer cells in select cases. Interestingly, the best IC50 value was obtained with the non-cyclized intermediate.
Açıklama
PMID: 34641289
WOS:000708237400001
WOS:000708237400001
Anahtar Kelimeler
Breast cancer, Furoindole, HDAC inhibitors, Neuroblastoma, SAHA enhancement
Kaynak
Molecules
WoS Q Değeri
Q2
Scopus Q Değeri
Q1
Cilt
26
Sayı
19
Künye
Bingül, M., Arndt, G. M., Marshall, G. M., St. Black, D. C.C., Cheung, B. ve Kumar, N. S. (2021). Synthesis and characterisation of novel tricyclic and tetracyclic furoindoles: Biological evaluation as SAHA enhancer against neuroblastoma and breast cancer cells. Molecules, 26(19), 5745.
