| Yazarlar |
Bathélémy Ngameni
Türkiye |
|
Kamdoum Cedric
Türkiye |
|
Armelle T. Mbaveng
Türkiye |
Doç. Dr. Musa ERDOĞAN
Kafkas Üniversitesi, Türkiye |
|
Ingrid Simo
Türkiye |
|
Victor Kuete
Türkiye |
|
Arif Daştan
Atatürk Üniversitesi, Türkiye |
| Özet |
| A new series of O-substituted chalcone derivatives bearing an/a allyl-, prenyl- or propargyl-substituent at different positions of rings A and B and their derivatives as drug leads, was designed, synthesized, and characterized. The chalcone derivatives were synthesized via base catalyzed Claisen-Schmidt condensation in MeOH or EtOH solutions of appropriately substituted aromatic ketones with O-allyl, and O-propargylvanillin, respectively. The intermediates O-substituted phenylketone derivatives were firstly synthesized by nucleophilic substitution reaction. All the newly synthesized compounds were characterized by IR, NMR spectral data and elemental analyses. A preliminary cytotoxicity was performed with the compounds (1a, 1b, 2a, 2b, 3a, 3b, 4a, 5a-f, 6a-d, 7a-d) and the positive control, doxorubicin towards CCRF-CEM leukemia cells. Amongst them, compounds 1a, 2a, 5b-d, 6b, 7a, 7c and doxorubicin displayed IC50 values below 20 µM while other compounds were less or not active at up to 50 µM. Remarkably interesting cytotoxic effects, with IC50 values below 1 µM were recorded with 5c against HCT116 p53-/- colon adenocarcinoma cells, 5e against CCRF-CEM cells and MDA-MB-231-BCRP breast adenocarcinoma cells, and 6b against HCT116 p53+/+ cells and HCT116 p53-/- cells. |
| Anahtar Kelimeler |
| 4-O-substituted chalcones | 4-O-substituted phenylcarbonyls | Anticancer activity | Claisen-Schmidt condensation | Nucleophilic O-substitution reaction | Synthesis |
| Makale Türü | Özgün Makale |
| Makale Alt Türü | SSCI, AHCI, SCI, SCI-Exp dergilerinde yayımlanan tam makale |
| Dergi Adı | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS |
| Dergi ISSN | 0960-894X |
| Dergi Tarandığı Indeksler | SCI-Expanded |
| Dergi Grubu | Q2 |
| Makale Dili | İngilizce |
| Basım Tarihi | 03-2021 |
| Cilt No | 35 |
| Sayı | 1 |
| Sayfalar | 127827 / 0 |
| Doi Numarası | 10.1016/j.bmcl.2021.127827 |
| Makale Linki | http://dx.doi.org/10.1016/j.bmcl.2021.127827 |
| Atıf Sayıları | |
| SCOPUS | 29 |
| Google Scholar | 38 |
