Design, synthesis, characterization, and anticancer activity of a novel series of O-substituted chalcone derivatives
Yazarlar (7)
Bathélémy Ngameni
Université De Yaoundé I, Kamerun
Kamdoum Cedric
Université De Yaoundé I, Kamerun
Armelle T. Mbaveng
University Of Dschang, Kamerun
Doç. Dr. Musa ERDOĞAN
Kafkas Üniversitesi, Türkiye
Ingrid Simo
University Of Dschang, Kamerun
Victor Kuete
University Of Dschang, Kamerun
Arif Daştan
Atatürk Üniversitesi, Türkiye
| Makale Türü | Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale) | ||
| Dergi Adı | Bioorganic and Medicinal Chemistry Letters (Q2) | ||
| Dergi ISSN | 0960-894X Wos Dergi Scopus Dergi | ||
| Dergi Tarandığı Indeksler | SCI-Expanded | ||
| Makale Dili | İngilizce | Basım Tarihi | 03-2021 |
| Cilt / Sayı / Sayfa | 35 / 1 / 127827–0 | DOI | 10.1016/j.bmcl.2021.127827 |
| Makale Linki | http://dx.doi.org/10.1016/j.bmcl.2021.127827 | ||
| 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 |
Science Direct
Design, synthesis, characterization, and anticancer activity of a novel series of O-substituted chalcone derivatives
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| SCOPUS | 43 |
| Google Scholar | 51 |