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Pregled bibliografske jedinice broj: 568529

New Sorafenib Derivatives: Synthesis, Antiproliferative Activity Against Tumour Cell Lines and Antimetabolic Evaluation


Babić, Željka; Crkvenčić, Maja; Rajić, Zrinka; Mikecin, Ana-Matea; Kralj, Marijeta; Balzarini, Jan; Petrova, Mariya; Vanderleyden, Jos; Zorc, Branka
New Sorafenib Derivatives: Synthesis, Antiproliferative Activity Against Tumour Cell Lines and Antimetabolic Evaluation // Molecules, 17 (2012), 1; 1124-1137 doi:10.3390/molecules17011124 (međunarodna recenzija, članak, znanstveni)


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Naslov
New Sorafenib Derivatives: Synthesis, Antiproliferative Activity Against Tumour Cell Lines and Antimetabolic Evaluation

Autori
Babić, Željka ; Crkvenčić, Maja ; Rajić, Zrinka ; Mikecin, Ana-Matea ; Kralj, Marijeta ; Balzarini, Jan ; Petrova, Mariya ; Vanderleyden, Jos ; Zorc, Branka

Izvornik
Molecules (1420-3049) 17 (2012), 1; 1124-1137

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

Ključne riječi
sorafenib ; amides ; cytostatic activity ; antimetabolic activity ; Caco-2 cells

Sažetak
Sorafenib is a relatively new cytostatic drug approved for the treatment of renal cell and hepatocellular carcinoma. In this report we describe the synthesis of sorafenib derivatives 4a–e which differ from sorafenib in their amide part. A 4-step synthetic pathway includes preparation of 4-chloropyridine-2-carbonyl chloride hydrochloride (1), 4-chloropyridine- 2-carboxamides 2a–e, 4-(4-aminophenoxy)-pyridine-2-carboxamides 3a–e and the target compounds 4-4-4-chloro-3-(trifluoromethyl)phenylcarbamoylamino-phenoxy- pyridine-2-carboxamides 4a–e. All compounds were fully chemically characterized and evaluated for their cytostatic activity against a panel of carcinoma, lymphoma and leukemia tumour cell lines. In addition, their antimetabolic potential was investigated as well. The most prominent antiproliferative activity was obtained for compounds 4a–e (IC50 = 14.3 μmol·L−1). Their potency was comparable to the potency of sorafenib, or even better. The compounds inhibited DNA, RNA and protein synthesis to a similar extent and did not discriminate between tumour cell lines and primary fibroblasts in terms of their anti-proliferative activity.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Temeljne medicinske znanosti, Farmacija



POVEZANOST RADA


Projekt / tema
006-0000000-3216 - Sinteza, karakterizacija i djelovanje potencijalnih i poznatih ljekovitih tvari (Zorc, Branka, MZOS)
098-0982464-2514 - Uloga različitih mehanizama odgovora stanica na terapiju oštećenjem DNA (Kralj, Marijeta, MZOS)

Ustanove
Farmaceutsko-biokemijski fakultet, Zagreb,
Institut "Ruđer Bošković", Zagreb

Citiraj ovu publikaciju

Babić, Željka; Crkvenčić, Maja; Rajić, Zrinka; Mikecin, Ana-Matea; Kralj, Marijeta; Balzarini, Jan; Petrova, Mariya; Vanderleyden, Jos; Zorc, Branka
New Sorafenib Derivatives: Synthesis, Antiproliferative Activity Against Tumour Cell Lines and Antimetabolic Evaluation // Molecules, 17 (2012), 1; 1124-1137 doi:10.3390/molecules17011124 (međunarodna recenzija, članak, znanstveni)
Babić, Ž., Crkvenčić, M., Rajić, Z., Mikecin, A., Kralj, M., Balzarini, J., Petrova, M., Vanderleyden, J. & Zorc, B. (2012) New Sorafenib Derivatives: Synthesis, Antiproliferative Activity Against Tumour Cell Lines and Antimetabolic Evaluation. Molecules, 17 (1), 1124-1137 doi:10.3390/molecules17011124.
@article{article, year = {2012}, pages = {1124-1137}, DOI = {10.3390/molecules17011124}, keywords = {sorafenib, amides, cytostatic activity, antimetabolic activity, Caco-2 cells}, journal = {Molecules}, doi = {10.3390/molecules17011124}, volume = {17}, number = {1}, issn = {1420-3049}, title = {New Sorafenib Derivatives: Synthesis, Antiproliferative Activity Against Tumour Cell Lines and Antimetabolic Evaluation}, keyword = {sorafenib, amides, cytostatic activity, antimetabolic activity, Caco-2 cells} }

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


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