Naslov
INHIBITORI POLIMERIZACIJE TUBULINA TEMELJENI NA N- BENZIMIDAZOLU I IMIDAZO[4,5-b]PIRIDINU
(N-BENZIMIDAZOLE AND IMIDAZO[4,5-b]PYRIDINE DERIVED TUBULINE POLYMERIZATION INHIBITORS)

Autori
Hranjec, Marijana

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

Izvornik
19th Ružička Days “Today Science – Tomorrow Industry” / Babić, Jurislav - Osijek : Zagreb : Prehrambeno tehnološki fakultet Sveučilišta Josipa Jurja Strossmayera u Osijeku ; Hrvatsko društvo kemijskih inženjera i tehnologa (HDKI), 2022, 2-2

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

Mjesto i datum
Vukovar, Hrvatska, 21.09.2022. - 23.09.2022

Vrsta sudjelovanja
Plenarno

Vrsta recenzije
Recenziran

Ključne riječi
benzimidazoli, imidazo[4, 5-b]piridini, tubulini, antitumorska aktivnost
(benzimidazoles, imidazo[4, 5-b]pyridines, tubulines, antitumor activity)

Sažetak
Nitrogen heterocycles, due to their widespread applications and interesting chemical, biological and pharmacological features, are nowadays still contributing extensively in the current organic and medicinal chemistry in the rational design of novel biologically active molecules [1]. Benzazole scaffold has become a fundamental building block widely incorporated in the structure of numerous natural, and synthetic molecules displaying versatile biological activities [2]. The structural similarity of benzimidazole and imidazo[4, 5-b]pyridine nuclei with natural purines, allowed their optimization to obtain more efficient and selective molecules which could play a crucial role in the function of many biologically important molecules, being thus of particular interest in pharmaceutical industry. Within this lecture, I will present the design, synthesis, and antiproliferative activity in vitro of novel N-benzimidazole and imidazo[4, 5- b]pyridine derived acrylonitriles [3, 4]. The chosen lead compounds were tested in vitro for tubulin polymerization inhibition as a possible mechanism of biological action. Immunofluorescence staining and tubulin polymerization assays confirmed tubulin as the main target which was also supported by the computational analysis. In addition, some compounds have proven to be very selective, non-cytotoxic and thus, a very promissing antitumoral agents for further investigation.

Izvorni jezik
Engleski

Znanstvena područja
Kemija

POVEZANOST RADA