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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
Dátum:	2014
ISSN:	0223-5234
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 folyóiratcikk Noscapine Antimicrotubule agents Apoptosis 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 OTKA TÁMOP-4.2.4.A/2-11/1-2012-0001 TÁMOP
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001-es BibID:	BIBFORM017684
Első szerző:	Reinart, Reet
Cím:	New 2-thioether-substituted apomorphines as potent and selective dopamine D2 receptor agonists / Reet Reinart, Zsuzsanna Gyulai, Sándor Berényi, Sándor Antus, Argo Vonk, Ago Rinken, Attila Sipos
Dátum:	2011
Megjegyzések:	A set of novel apomorphine derivatives were synthesized with diversely functionalized side chains in the proximity of position 2 of the aporphine skeleton. Amino and/or carboxylic functions were introduced to this region of the backbone to test their pharmacological effects. During the synthesis of 2-(S-3-mercaptopropionic acid)-derivative a heteroring-fused congener was also isolated. The structural elucidation confirmed that the formation of this product was in accordance with our previous observations on the reaction of thebaine (2) with thiosalycilic acid. All the novel apomorphine congeners 4aeg were neuropharmacologically characterized to discover their dopaminergic profiles. Two derivatives were identified as D2 full agonists equipotent with apomorphine (1) having significantly increased D2/D1 selectivity ratios.
Tárgyszavak:	Természettudományok Kémiai tudományok idegen nyelvű folyóiratközlemény külföldi lapban Apomorphine derivatives Parkinson's disease Structure-activity relationship Dopamine receptor activity Subtype selectivity
Megjelenés:	European Journal of Medicinal Chemistry. - 46 : 7 (2011), p. 2992-2999. -
További szerzők:	Gyulai Zsuzsanna Berényi Sándor (1947-2019) (szerves kémikus) Antus Sándor (1944-2022) (vegyészmérnök) Vonk, Argo Rinken, Ago Sipos Attila (1977-) (vegyész, angol-magyar szakfordító)
Pályázati támogatás:	K81701 OTKA
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