Naslov
Cytotoxicity of harmiquines, hybrids based on harmine and chloroquine scaffolds

Autori
Poje, Goran ; Held, Jana ; Rajić, Zrinka

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

Izvornik
27th Croatian Meeting of Chemists and Chemical Engineers, Book of Abstracts / Marković, Dean ; Meštrović, Ernest ; Namjesnik, Danijel ; Tomašić, Vesna - Zagreb : Hrvatsko kemijsko društvo, 2021, 236-236

Skup
27. hrvatski skup kemičara i kemijskih inženjera (27HSKIKI)

Mjesto i datum
Veli Lošinj, Hrvatska, 05.10.2021. - 08.10.2021

Vrsta sudjelovanja
Poster

Vrsta recenzije
Domaća recenzija

Ključne riječi
malaria, hybrid compounds, harmine, chloroquine, cytotoxicity

Sažetak
Cancer, a disease characterized by uncontrolled growth of abnormal cells, is the second leading cause of death globally, accounting for an estimated 9.6 million deaths in 2018.[1] The emergence of cancer drug resistance remains a significant global public health and economic burden, emphasizing the need for new and effective anticancer agents. Herein, we represent harmiquines, hybrid compounds based on harmine and chloroquine, two moieties with confirmed anticancer properties.[2, 3] The cytotoxic potential of novel hybrids was examined in vitro against a panel of human cell lines (Hek293T, MCF-7, HepG2, SW620, HCT116). The cell growth rate was evaluated using the MTT assay with respect to untreated cells. Cytotoxicity, expressed as an IC50 value, was determined from concentration–response curve using nonlinear regression analysis. The compounds differentially affected the growth of tumor cell lines, whereby MCF-7 and HCT-116 cell lines appeared generally sensitive towards most of the tested compounds. Hybrids 1 and 2 (C-7-tethered derivatives) proved to be the most cytotoxic, affecting all tumor cell lines (IC50 values in the range of 1-8 μM) (Figure 1.). Harmiquine 3 exerted the most selective activity towards HepG2, in comparison to Hek293T (IC50 = 5.5 ± 3.2 uM, selectivity index > 9).

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Farmacija

POVEZANOST RADA