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Pregled bibliografske jedinice broj: 834206

Časopis

Autori: Perin, Nataša; Bobanović, Kristina; Zlatar, Ivo; Jelić, Dubravko; Kelava, Vanja; Koštrun, Sanja; Gabelica Marković, Vesna; Brajša, Karmen; Hranjec, Marijana
Naslov: Antiproliferative activity of amino substituted benzo[b]thieno[2, 3-b]pyrido[1, 2-a]benzimidazoles explored by 2D and 3D cell culture system
( Antiproliferative activity of amino substituted benzo[b]thieno[2, 3-b]pyrido[1, 2-a]benzimidazoles explored by 2D and 3D cell culture system )
Izvornik: European journal of medicinal chemistry (0223-5234) 125 (2017); 722-735
Vrsta rada: članak
Ključne riječi: antiproliferative activity ; benzo[b]thieno[2 ; 3-b]pyrido[1 ; 2-a]benzimidazoles ; 2D and 3D in vitro cytotoxicity assay ; lipophilicity ; physico-chemical properties
( antiproliferative activity ; benzo[b]thieno[2 ; 3-b]pyrido[1 ; 2-a]benzimidazoles ; 2D and 3D in vitro cytotoxicity assay ; lipophilicity ; physico-chemical properties )
Sažetak:
Benzimidazo[1, 2-a]quinolines and benzo[b]thieno[2, 3-b]pyrido[1, 2-a]benzimidazoles with amino chains on the different positions have been evaluated by 2D and 3D assays on the human breast cancer cells. Pentacyclic derivatives were synthesized by microwave assisted amination to study the influence of the thiophene substructure on antitumor activity in comparison to tetracyclic analogues. The results obtained from 2D assay reveals that the antitumor activity is strongly dependent on the nature and position of amino chains. Tetracyclic derivatives displayed selective activity on SK-BR-3 with the 2-amino substituted derivatives as the most active ones while pentacyclic derivatives 6-16 and 21-25 showed more pronounced activity on T47-D . The evaluation of antitumor activity in the 3D assay pointed out that some of the tetracyclic and pentacyclic amino substituted derivatives showed selective activity on the MDA-MB-231 cell line. Influence of physico-chemical properties of the compounds on antiproliferative activity have been investigated by multivariate statistical methods. As a measure of lipophilicity, experimental Chrom LogD values have been determined and number of structural parameters have been calculated for investigated compounds. Main factors contributing to the antiproliferative effect for both 2D and 3D cell cultures are found to be basicity, lipophilicity, molecular weight and number of H-bond donors.
Projekt / tema: HRZZ-IP-2013-11-5596
Izvorni jezik: eng
Rad je indeksiran u
bazama podataka:
Current Contents Connect (CCC)
MEDLINE
Scopus
SCI-EXP, SSCI i/ili A&HCI
Science Citation Index Expanded (SCI-EXP) (sastavni dio Web of Science Core Collectiona)
Kategorija: Znanstveni
Znanstvena područja:
Kemija,Temeljne medicinske znanosti
URL Internet adrese: http://www.sciencedirect.com/science/article/pii/S0223523416308200
Broj citata:
Altmetric:
DOI: 10.1016/j.ejmech.2016.09.084
URL cjelovitog teksta:
Google Scholar: Antiproliferative activity of amino substituted benzo[b]thieno[2, 3-b]pyrido[1, 2-a]benzimidazoles explored by 2D and 3D cell culture system
Upisao u CROSBI: Marijana Hranjec (mhranjec@fkit.hr), 26. Ruj. 2016. u 09:17 sati



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