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Pregled bibliografske jedinice broj: 384615

Časopis

Autori: Ester, Katja; Hranjec, Marijana; Piantanida, Ivo; Ćaleta, Irena; Ivana, Jarak; Pavelić, Krešimir; Kralj, Marijeta; Karminski-Zamola, Grace
Naslov: Novel Derivatives of Pyridyl-Benzo[b]thiophene-2-carboxamides and Benzo[b]thieno[2, 3- c]naphthyridin-2-ones: Minor Structural Variations Provoke Major Differences of Antitumor Action Mechanisms
Izvornik: Journal of Medicinal Chemistry (0022-2623) 52 (2009), 8; 2482-2492
Vrsta rada: članak
Ključne riječi: pyridyl-benzo b thiophene-2-carboxamides and benzo b thieno 2; 3-c naphthyridin-2-ones; DNA binding; anticancer activity; topoisomerase I inhibition; anti-tubulin activity; intercalators; minor groove
Sažetak:
Novel cyano- and 2-imidazolinyl-substituted derivatives of pyridyl-benzo[b]thiophene-2- carboxamides 4, 5, 10-13 and benzo[b]thieno[2, 3-c]naphthyridin-2-ones 6, 7, 14-17 were prepared. All derivatives showed prominent antiproliferative effect. Extensive DNA binding studies and additional biological evaluations point to various modes/targets of action. The results strongly support intercalation into DNA as a dominant binding mode of fused analogues, which was substantiated using topoisomerase I inhibition assay. Most intriguingly, only minor structural difference between non-fused compounds 12 and 13 has strong impact on the interactions with DNA: while 13 binds within the DNA minor groove in the form of dimer, 12 does not form significant interactions with DNA. The assumption that severe mitotic impairment (G2/M phase arrest) induced by 12 could point to another important target – tubulin was confirmed by its obvious anti-tubulin activity observed in immunofluorescence assay, whereby treated cells showed disruption of microtubule formation comparable to the effect obtained by Paclitaxel, well-known tubulin antagonist chemotherapeutic.
Projekt / tema: 098-0982464-2393, 098-0982914-2918, 098-0982464-2514, 125-0982464-1356
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 cjelovitog teksta:
Google Scholar: Novel Derivatives of Pyridyl-Benzo[b]thiophene-2-carboxamides and Benzo[b]thieno[2, 3- c]naphthyridin-2-ones: Minor Structural Variations Provoke Major Differences of Antitumor Action Mechanisms
Upisao u CROSBI: gkzam@fkit.hr (gkzam@fkit.hr), 10. Ožu. 2009. u 09:19 sati



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