Stereoselective Synthesis and Antiproliferative Activity of Steviol-Based Diterpene 1,3-Aminoalcohol Regioisomers

A series of novel diterpene-type 1,3-aminoalcohols and their regioisomers have been synthesised from natural stevioside in a stereoselective manner. The key intermediate β-keto alcohol was prepared using Wagner–Meerwein rearrangement of the epoxide derived from steviol methyl ester. The primary amin...

Teljes leírás

Elmentve itt :
Bibliográfiai részletek
Szerzők: Bai Dorottya
Schelz Zsuzsanna
Boncz Mária Fanni
Zupkó István
Szakonyi Zsolt
Dokumentumtípus: Cikk
Megjelent: 2023
Sorozat:MOLECULES 28 No. 24
Tárgyszavak:
doi:10.3390/molecules28247962

mtmt:34417276
Online Access:http://publicatio.bibl.u-szeged.hu/29006
LEADER 01994nab a2200265 i 4500
001 publ29006
005 20231207081024.0
008 231207s2023 hu o 0|| Angol d
022 |a 1420-3049 
024 7 |a 10.3390/molecules28247962  |2 doi 
024 7 |a 34417276  |2 mtmt 
040 |a SZTE Publicatio Repozitórium  |b hun 
041 |a Angol 
100 1 |a Bai Dorottya 
245 1 0 |a Stereoselective Synthesis and Antiproliferative Activity of Steviol-Based Diterpene 1,3-Aminoalcohol Regioisomers  |h [elektronikus dokumentum] /  |c  Bai Dorottya 
260 |c 2023 
300 |a 22 
490 0 |a MOLECULES  |v 28 No. 24 
520 3 |a A series of novel diterpene-type 1,3-aminoalcohols and their regioisomers have been synthesised from natural stevioside in a stereoselective manner. The key intermediate β-keto alcohol was prepared using Wagner–Meerwein rearrangement of the epoxide derived from steviol methyl ester. The primary aminoalcohol was formed via Raney-nickel-catalysed hydrogenation of an oxime, and a versatile library of aminoalcohols was synthesised using a Schiff base with the primary amines. The aminoalcohol regioisomers were prepared from the mesylate of the β-keto alcohols. The corresponding primary aminoalcohol was formed via the palladium-catalysed hydrogenation of hydroxyl-azide, and click reactions of the latter were also carried out. The new compounds were characterised using 1D- and 2D-NMR techniques and HRMS measurements. The in vitro investigations showed high inhibition of cell growth in human cancer cell lines (HeLa, SiHa, A2780, MCF-7 and MDA-MB-231) in the case of naphthalic N-substituted derivatives. The antiproliferative effects were assayed using the MTT method. 
650 4 |a Farmakológia és gyógyszerészet 
700 0 1 |a Schelz Zsuzsanna  |e aut 
700 0 1 |a Boncz Mária Fanni  |e aut 
700 0 1 |a Zupkó István  |e aut 
700 0 1 |a Szakonyi Zsolt  |e aut 
856 4 0 |u http://publicatio.bibl.u-szeged.hu/29006/1/Molecules_7962_Bai_2023.pdf  |z Dokumentum-elérés