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Pregled bibliografske jedinice broj: 1034130

Antiproliferative activity and mode of action analysis of novel amino and amido substituted phenantrene and naphtho[2, 1-b]thiophene derivatives


Perin, Nataša; Rep, Valentina; Sović, Irena; Juričić, Štefica; Selgrad, Danijel; Klobučar, Marko; Pržulj, Nataša; Gupta, Chhedi Lal Gupta; Malod-Dognin, Noel; Kraljević Pavelić, Sandra; Hranjec, Marijana
Antiproliferative activity and mode of action analysis of novel amino and amido substituted phenantrene and naphtho[2, 1-b]thiophene derivatives // European journal of medicinal chemistry, 185 (2020), 111833, 13 doi:10.1016/j.ejmech.2019.111833 (međunarodna recenzija, članak, znanstveni)


CROSBI ID: 1034130 Za ispravke kontaktirajte CROSBI podršku putem web obrasca

Naslov
Antiproliferative activity and mode of action analysis of novel amino and amido substituted phenantrene and naphtho[2, 1-b]thiophene derivatives

Autori
Perin, Nataša ; Rep, Valentina ; Sović, Irena ; Juričić, Štefica ; Selgrad, Danijel ; Klobučar, Marko ; Pržulj, Nataša ; Gupta, Chhedi Lal Gupta ; Malod-Dognin, Noel ; Kraljević Pavelić, Sandra ; Hranjec, Marijana

Izvornik
European journal of medicinal chemistry (0223-5234) 185 (2020); 111833, 13

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
amines ; amides ; antiproliferative activity ; phenatrenes ; mode of action analysis ; naphtho[2, 1-b]thiophenes

Sažetak
Herein we present and describe the design and synthesis of novel phenantrene derivatives substituted with either amino or amido side chains and their biological activity. Antiproliferative activities were assessed in vitro on a panel of human cancer cell lines. Tested compounds showed moderate activity against cancer cells in comparison with 5- fluorouracile. Among all tested compounds, some compounds substituted with cyano groups showed a pronounced and selective activity in the nanomolar range of inhibitory concentrations against HeLa and HepG2. The strongest selective activity against HeLa cells was observed for acrylonitriles 8 and 11 and their cyclic analogues 15 and 17 substituted with two cyano groups with a corresponding IC50 = 0.33, 0.21, 0.65 and 0.45 M, respectively. Compounds 11 showed the most pronounced selectivity being almost non cytotoxic to normal fibroblasts. Additionally, mode of biological action analysis was performed in silico and in vitro by Western blot analysis of HIF-1-α relative expression for compounds 8 and 11.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Biologija, 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) ( POIROT)

Ustanove:
Fakultet kemijskog inženjerstva i tehnologije, Zagreb,
Sveučilište u Rijeci - Odjel za biotehnologiju

Citiraj ovu publikaciju

Perin, Nataša; Rep, Valentina; Sović, Irena; Juričić, Štefica; Selgrad, Danijel; Klobučar, Marko; Pržulj, Nataša; Gupta, Chhedi Lal Gupta; Malod-Dognin, Noel; Kraljević Pavelić, Sandra; Hranjec, Marijana
Antiproliferative activity and mode of action analysis of novel amino and amido substituted phenantrene and naphtho[2, 1-b]thiophene derivatives // European journal of medicinal chemistry, 185 (2020), 111833, 13 doi:10.1016/j.ejmech.2019.111833 (međunarodna recenzija, članak, znanstveni)
Perin, N., Rep, V., Sović, I., Juričić, Š., Selgrad, D., Klobučar, M., Pržulj, N., Gupta, C., Malod-Dognin, N., Kraljević Pavelić, S. & Hranjec, M. (2020) Antiproliferative activity and mode of action analysis of novel amino and amido substituted phenantrene and naphtho[2, 1-b]thiophene derivatives. European journal of medicinal chemistry, 185, 111833, 13 doi:10.1016/j.ejmech.2019.111833.
@article{article, year = {2020}, pages = {13}, DOI = {10.1016/j.ejmech.2019.111833}, chapter = {111833}, keywords = {amines, amides, antiproliferative activity, phenatrenes, mode of action analysis, naphtho[2, 1-b]thiophenes}, journal = {European journal of medicinal chemistry}, doi = {10.1016/j.ejmech.2019.111833}, volume = {185}, issn = {0223-5234}, title = {Antiproliferative activity and mode of action analysis of novel amino and amido substituted phenantrene and naphtho[2, 1-b]thiophene derivatives}, keyword = {amines, amides, antiproliferative activity, phenatrenes, mode of action analysis, naphtho[2, 1-b]thiophenes}, chapternumber = {111833} }
@article{article, year = {2020}, pages = {13}, DOI = {10.1016/j.ejmech.2019.111833}, chapter = {111833}, keywords = {amines, amides, antiproliferative activity, phenatrenes, mode of action analysis, naphtho[2, 1-b]thiophenes}, journal = {European journal of medicinal chemistry}, doi = {10.1016/j.ejmech.2019.111833}, volume = {185}, issn = {0223-5234}, title = {Antiproliferative activity and mode of action analysis of novel amino and amido substituted phenantrene and naphtho[2, 1-b]thiophene derivatives}, keyword = {amines, amides, antiproliferative activity, phenatrenes, mode of action analysis, naphtho[2, 1-b]thiophenes}, chapternumber = {111833} }

Časopis indeksira:


  • Current Contents Connect (CCC)
  • Web of Science Core Collection (WoSCC)
    • Science Citation Index Expanded (SCI-EXP)
    • SCI-EXP, SSCI i/ili A&HCI
  • Scopus
  • MEDLINE


Uključenost u ostale bibliografske baze podataka:


  • BIOSIS Previews (Biological Abstracts)


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