Pregled bibliografske jedinice broj: 1009719
Synthesis and biological activity of novel N- substituted benzimidazole acrylonitriles
Synthesis and biological activity of novel N- substituted benzimidazole acrylonitriles // Book of Abstracts, Joint Meeting on Medicinal Chemistry, Prague, 2019 / Vinšová, Jarmila (ur.).
Prag: GUARANT International spol. s r.o., 2019. str. 71-71 (poster, međunarodna recenzija, sažetak, znanstveni)
CROSBI ID: 1009719 Za ispravke kontaktirajte CROSBI podršku putem web obrasca
Naslov
Synthesis and biological activity of novel N- substituted benzimidazole acrylonitriles
Autori
Hranjec, Marijana ; Perin, Nataša ; Beč, Anja ; Persoons, Lentje ; Daelemans, Dirk
Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni
Izvornik
Book of Abstracts, Joint Meeting on Medicinal Chemistry, Prague, 2019
/ Vinšová, Jarmila - Prag : GUARANT International spol. s r.o., 2019, 71-71
ISBN
978-80-907442-0-2
Skup
11th Joint Meeting on Medicinal Chemistry 2019
Mjesto i datum
Prag, Češka Republika, 27.06.2019. - 30.06.2019
Vrsta sudjelovanja
Poster
Vrsta recenzije
Međunarodna recenzija
Ključne riječi
acrylonitriles, benzimidazoles, antiproliferative activity
Sažetak
Small heteroaromatic molecules, like nitrogen- containing heterocycles play an important role in medicinal chemistry due to variety of their possible chemical, pharmacological and industrial applications. Benzimidazole structural motifs, as an important bioactive heterocyclic building block in medicinal chemistry, are widely incorporated in the structure of numerous natural or synthetic medical and biochemical molecules possessing versatile biological features.[1, 2] Within this work, we would like to present the synthesis and biological activity of novel N- substituted benzimidazole based acrylonitriles. For the synthesis of novel compounds we have used methods of classical linear organic synthesis as well as microwave assisted synthesis starting from aromatic benzaldehydes and substituted 1, 2- phenylenediamnies.[3] All newly prepared compounds were tested for their antiproliferative activity in vitro on nine human cancer as well as non cancerous cell lines. Some of compounds showed strong and selective antiproliferative activity in submicromolar range of IC50 concentrations. Additional experiments showed that some compounds did not affect normal cells. Mechanism of action studies demonstrated that two most active compounds inhibited the polymerisation of tubuline.
Izvorni jezik
Engleski
Znanstvena područja
Kemija, Temeljne medicinske znanosti
POVEZANOST RADA
Projekti:
HRZZ-IP-2018-01-4379 - Istraživanje antioksidativnog djelovanja benzazolskog skeleta u dizajnu novih antitumorskih agensa (AntioxPot) (Hranjec, Marijana, HRZZ - 2018-01) ( CroRIS)
Ustanove:
Fakultet kemijskog inženjerstva i tehnologije, Zagreb