Összesen 2 találat.


001-es BibID:BIBFORM040261
Első szerző:Gyulai Zsuzsanna
Cím:Synthesis and Opioid Activity of Novel 6-ketolevorphanol Derivatives / Zsuzsanna Gyulai, Antal Udvardy, Attila Cs. Bényei, Jakub Fichna, Katarzyna Gach, Martin Storr, Géza Tóth, Sándor Antus, Sándor Berényi, Anna Janecka, Attila Sipos
Megjegyzések:Novel 6-ketolevorphanol analogs with diverse substitution patterns at ring C were synthesized and their binding affinities at the ?, ? and ? opioid receptors were investigated. The in vitro activity of the new analogs was then evaluated in the functional assay based on the electrically-stimulated contractions of the mouse ileum. It was shown that analogs with ?7,8 bond had no significant potency at any of the opioid receptor types. In contrast, analogs with the saturated ring C were either potent ? agonist or antagonist depending on the absence or presence of the hydroxyl group in position 14.
Tárgyszavak:Természettudományok Kémiai tudományok idegen nyelvű folyóiratközlemény külföldi lapban
Opioid receptors
Binding Assay
Doktori iskola
Megjelenés:Medicinal Chemistry. - 9 (2013), p. 1-10. -
További szerzők:Udvardy Antal (1981-) (vegyész) Bényei Attila (1962-) (vegyész) Fichna, Jakub Gach, Katarzyna Storr, Martin Tóth Géza Antus Sándor (1944-2022) (vegyészmérnök) Berényi Sándor (1947-2019) (szerves kémikus) Janecka, Anna Sipos Attila (1977-) (vegyész, angol-magyar szakfordító)
Pályázati támogatás:K68482, K81701, 101372
Fizikai Tudományok Doktori Iskola
Internet cím:Intézményi repozitóriumban (DEA) tárolt változat
Szerző által megadott URL 856 41


001-es BibID:BIBFORM055222
Első szerző:Porcù, Elena
Cím:Novel 9'-substituted-noscapines : synthesis with Suzuki cross-coupling, structure elucidation and biological evaluation / Elena Porcù, Attila Sipos, Giuseppe Basso, Ernest Hamel, Ruoli Bai, Verena Stempfer, Antal Udvardy, Attila Cs. Bényei, Helmut Schmidhammer, Sándor Antus, Giampietro Viola
Megjegyzések:Tubulin is a major molecular target for anticancer drugs. The dynamic process of microtubule assembly and disassembly can be blocked by various agents that bind to distinct sites on tubulin, usually its ?-subunit. Among the antimitotic agents that perturb microtubule dynamics, noscapinoids represent an emerging class of agents. In particular, 9'-bromonoscapine (EM011) has been identified as a potent noscapine analog. Here we present high yielding, efficient synthetic methods based on Suzuki coupling of 9'-alkyl and 9'-arylnoscapines and an evaluation of their antiproliferative properties. Our results showed that 9'-alkyl and 9'-aryl derivatives inhibit proliferation of human cancer cells. The most active compounds were the 9'-methyl and the 9'-phenyl derivatives, which showed similar cytotoxic potency in comparison to the 9'-brominated derivative. Interestingly these newly synthesized derivatives did not induce cell death in normal human lymphocytes, suggesting that the compounds may be selective against cancer cells. All of these derivatives, except 9'-(2-methoxyphenyl)-noscapine, efficiently induced a cell cycle arrest in the G2/M phase of the cell cycle in HeLa and Jurkat cells. Furthermore, we showed that the most active compounds in HeLa cells induced apoptosis following the mitochondrial pathway with the activation of both caspase-9 and caspase-3. In addition, these compounds significantly reduced the expression of the anti-apoptotic proteins Mcl-1 and Bcl-2.
Tárgyszavak:Természettudományok Kémiai tudományok idegen nyelvű folyóiratközlemény külföldi lapban
Antimicrotubule agents
Cell cycle arrest
Suzuki reaction
Megjelenés:European Journal of Medicinal Chemistry. - 84 (2014), p. 476-490. -
További szerzők:Sipos Attila (1977-) (vegyész, angol-magyar szakfordító) Basso, Giuseppe Hamel, Ernest Bai, Ruoli Stempfer, Verena Udvardy Antal (1981-) (vegyész) Bényei Attila (1962-) (vegyész) Schmidhammer, Helmut Antus Sándor (1944-2022) (vegyészmérnök) Viola, Giampietro
Pályázati támogatás:101372
Internet cím:Szerző által megadott URL
Intézményi repozitóriumban (DEA) tárolt változat
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