Naslov
Harmicenes, harmine-ferrocene hybrids, as novel anticancer agents
(Harmicenes, harmine-ferrocene hybrids, as novel anticancer agents)

Autori
Poje, Goran ; Marinović, Marina ; Rajić, Zrinka

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

Izvornik
EFMC-ISMC International Symposium on Medicinal Chemistry, Book of Abstracts / - Nica : EFMC, 2022, 250-250

Skup
27th EFMC International Symposium on Medicinal Chemistry 2022 (EFMC-ISMC)

Mjesto i datum
Nica, Francuska, 04.09.2022. - 08.09.2022

Vrsta sudjelovanja
Poster

Vrsta recenzije
Međunarodna recenzija

Ključne riječi
cancer, harmine, ferrocene, hybrid molecules, antiproliferative activity

Sažetak
Cancer, a group of diseases characterized by the uncontrolled growth and spread of abnormal cells, is one of the leading causes of death worldwide, accounting for nearly 10 million deaths in 2020 (1). In recent decades, it has become evident that cancer cells can develop multidrug resistance to conventional anticancer drugs, leading to tumor reccurence. Therefore, there is a constant need for the discovery of new and effective anticancer drugs (2). Our ongoing efforts in the search for novel hybrid molecules with anticancer activity have resulted in a series of harmicenes – novel hybrids comprising two moieties with anticancer properties (3, 4), namely harmine and ferrocene, linked via a 1, 2, 3-triazole or amide bond. The cytotoxic potential of the new hybrids was evaluated in vitro against a panel of human tumor cell lines (Hek293T, MCF-7, HepG2, SW620, HCT116). The cell growth rate was assessed by MTT assay with respect to untreated cells. Cytotoxicity, expressed as IC50 value, was determined from the concentration-response curve by linear regression analysis. Compounds 1 and 2 (C-6- and C-7-tethered derivatives, respectively) showed remarkable cytotoxic activities against all tumor cell lines studied with low micromolar IC50 values (< 10 µM). On the other hand, harmicenes bearing substituent at the position N-9 of the β-carboline core exhibited the poorest cytotoxic activities, with exception of compound 3 which showed moderate activity against MCF-7, SW620 and HCT116 cell lines. Compounds 4 and 5 (triazole-type derivatives) showed selectivity toward HCT116. All tested hybrids, except compounds 1 and 2, were found to be inactive against Hek293T. Further research will focus on determining harmicenes' mechanism of action.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Farmacija

POVEZANOST RADA