Naslov
Synthesis and antiproliferative activity of the novel 1, 2, 3-triazole coumarin and quinoline derivatives

Autori
Sokol, Ivana ; Krnić, Mia ; Liekens, Sandra ; Raić-Malić, Silvana ; Gazivoda Kraljević, Tatjana

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni

Izvornik
Book of abstracts International conference 17th Ružička Days "Today Science - Tomorrow Industry" / Tomas, Srećko ; Ačkar, Đurđica - Zagreb : Hrvatsko društvo kemijskih inženjera i tehnologa (HDKI), 2018, 93-93

ISBN
978-953-6894-65-9

Skup
17. Ružičkini dani "Danas znanost - sutra industrija"

Mjesto i datum
Vukovar, Hrvatska, 19.09.2018. - 21.09.2018

Vrsta sudjelovanja
Poster

Vrsta recenzije
Međunarodna recenzija

Ključne riječi
1, 2, 3-triazole, coumarin, quioline, click reaction, antiproliferative activity

Sažetak
1, 2, 3-triazole ring has a great role as pharmacophore which is responsible for antitumor and antimicrobial activity. It is introduced in many drugs due to moderate dipole properties, rigid structure and stability in vivo. Besides, 1, 2, 3-triazoles have attracted considerable attention in recent years because of their wide range of biological activities against various viruses, malignant cells, microorganisms and their inhibitory activities against several enzymes Furthermore, coumarin–1, 2, 3-triazole–benzofused heterocycle hybrids emerged as the class of compounds exhibiting the highest antiproliferative activity. In order to evaluate antiproliferative activity of novel compounds against human lymphoblastic leukemia cells (CEM/C1), human cervix carcinoma cells (HeLa) and human dermal microvascular endothelial cells (HMEC-1), the novel 1, 2, 3-triazole derivatives of coumarin and quinoline have been synthesized by click reaction of 3-azido-7-hydroxycoumarin or 4-azidoquinoline with corresponding terminal acetylenes in the presence of copper as a catalyst. Antiproliferative activity evaluation of the novel compounds showed that 1, 2, 3-triazole coumarin derivative with 3, 5-ditrifluoromethylphenyl substituent exhibited the most pronounced activity against HeLa cell lines (IC50=9.9 µM). [1] S. Raić-Malić, A. Meščić, Curr. Med. Chem. 22 (2015) 1462. [2] T. Gazivoda Kraljević, A. Harej, M. Sedić, S. Kraljević Pavelić, V. Stepanić, D. Drenjančević, J. Talapko, S. Raić-Malić, Eur. J. Med. Chem. 124 (2016) 794.

Izvorni jezik
Engleski

Znanstvena područja
Kemija

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