Naslov
Synthesis of novel 3-substituted coumarin derivatives by transition metal-catalyzed reactions and their antimicrobial and antitumoral evaluations

Autori
Sokol, Ivana ; Meščić Macan, Andrijana ; Drenjančević, Domagoj ; Liekens, Sandra ; Raić-Malić, Silvana ; Gazivoda Kraljević, Tatjana

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, ostalo, ostalo

Izvornik
Chemistry World Conference / - , 2021

Skup
Chemistry World Conference 2021

Mjesto i datum
Rim, Italija, 06.09.2021. - 07.09.2021

Vrsta sudjelovanja
Poster

Vrsta recenzije
Međunarodna recenzija

Ključne riječi
coumarin, Pd-catalysed reaction, click reaction, antibacterial, antitumor

Sažetak
Coumarin has an important place in medicinal chemistry, as molecules incorporating the coumarin scaffold show a broad spectrum of pharmacological activities, including anticancer, antimicrobial, antiviral, antioxidant, anticoagulant, anti-inflammatory, and anti-enzymatic. The aim of our study was to synthesise new coumarin-based compounds by using transition metal-catalysed reactions and evaluate their antibacterial and antitumor potential. A series of 7-hydroxycoumarin derivatives with aliphatic and aryl moiety attached directly at C-3 of coumarin ring and through the ethynyl or 1, 2, 3-triazole linker were prepared by Pd-catalysed or click reaction. The 3-substituted coumarin derivative bearing bistrifluoromethylphenyl at the C-4 position of 1, 2, 3-triazole showed strong and selective antiproliferative activity against cervix adenocarcinoma (HeLa) cells. The 7-hydroxy-4-methylcoumarin with a phenyl ring directly attached to coumarin at C-3 showed good potency against MRSA and VRE strains. The promising antiproliferative activity of coumarin derivative bearing 3, 5-ditrifluoromethylphenyl substituent and antibacterial activity of coumarin derivative with aromatic moiety suggest that further enhancements could be obtained by structural optimisation of the coumarin core.

Izvorni jezik
Engleski

Znanstvena područja
Kemija

POVEZANOST RADA