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Pregled bibliografske jedinice broj: 572747

Časopis

Autori: Wittine, Karlo; Stipković Babić, Maja; Makuc, Damjan; Plavec, Janez; Kraljević Pavelić, Sandra; Sedić, Mirela; Pavelić, Krešimir; Leyssene, Pieter; Neytse, Johan; Balzarinie, Jan; Mintas, Mladen
Naslov: Novel 1, 2, 4-Triazole and Imidazole Derivatives of L-Ascorbic and Imino-Ascorbic Acid: Synthesis, Anti-HCV and Antitumor Activity Evaluations
Izvornik: Bioorganic & medicinal chemistry (0968-0896) 20 (2012), 11; 3675-3685
Vrsta rada: članak
Ključne riječi: 1; 2; 4-triazole; imidazole; L-ascorbic acid; anti-HCV activity; antitumor activity; IMPDH
Sažetak:
Several novel 1, 2, 4-triazole and imidazole L- ascorbic acid (1, 2, 3, 5, 6 and 9) and imino- ascorbic acid (4, 7 and 8) derivatives were prepared and evaluated for their inhibitory activity against hepatitis C virus (HCV) replication and human tumour cell proliferation. Compounds 6 and 9 exerted the most pronounced cytostatic effects in all tumour cell lines tested, and were highly selective for human T-cell acute lymphoblastic leukaemia cells (CEM/0) with IC50s of 104 and 7.30.1 µM, respectively. Unlike compound 9, compound 6 showed no toxicity in human diploid fibroblasts. One of the possible mechanisms of action of compound 6 accounting for observed cytostatic activity towards haematological malignancies might be inhibition of inosine monophosphate dehydrogenase (IMPDH) activity, a key enzyme of de novo purine nucleotide biosynthesis providing the cells with precursors for DNA and RNA synthesis indispensable for cell growth and division, which has emerged as an important target for antileukemic therapy. In addition, this compound proved to be the most potent inhibitor of the hepatitis C virus replication as well. However, observed antiviral effect was most likely associated with the effect that the compound exerted on the host cell rather than with selective effect on the replication of the virus itself. In conclusion, results of this study put forward compound 6 as a potential novel antitumor agent (IMPDH inhibitor) for treating leukaemia. Its significant biological activity and low toxicity in human diploid fibroblasts encourage further development of this compound as a lead.
Projekt / tema: 335-0000000-3532, 335-0982464-2393, 125-098-2464-2922
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://dx.doi.org/10.1016/j.bmc.2012.01.054
http://www.sciencedirect.com/science/article/pii/S0968089612001010
http://ac.els-cdn.com/S0968089612001010/1-s2.0-S0968089612001010-main.pdf?_tid=cf846a80-c6d4-11e2-a02e-00000aacb35e&acdnat=1369662989_58da936b06544386cfce36d2cd4fdb23
Broj citata:
Altmetric:
DOI: 10.1016/j.bmc.2012.01.054
URL cjelovitog teksta: http://dx.doi.org/10.1016/j.bmc.2012.01.054
Google Scholar: Novel 1, 2, 4-Triazole and Imidazole Derivatives of L-Ascorbic and Imino-Ascorbic Acid: Synthesis, Anti-HCV and Antitumor Activity Evaluations
Upisao u CROSBI: sandrakp@uniri.hr (sandrakp@uniri.hr), 1. Ožu. 2012. u 10:48 sati



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