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A tryptophanol-derived oxazolopiperidone lactam is cytotoxic against tumors via inhibition of p53 interaction with murine double minute proteins.
Enantioselective Synthesis of Indole Alkaloids from Chiral Lactams
This account reports on the use of (R)- or (S)-phenylglycinol- and (S)-tryptophanol-derived oxazolopiperidone lactams as building blocks for the enantioselective synthesis of structurally diverse…
Indolo[2,3-a]quinolizidines and Derivatives: Bioactivity and Asymmetric Synthesis.
- Maria Pérez, Margarida Espadinha, Maria M. M. Santos
- Chemistry, BiologyCurrent pharmaceutical design
- 31 October 2015
The main biological effects described for indoloquinolizidines include analgesic, anti-inflammatory, antihypertensive, and antiarrhythmic activities, as well as inhibition of multiple ion channels, affinity for opioid receptors, and activity against Leishmania.
Stereocontrolled Annulations of Indolo[2,3-a]quinolizidine-Derived Lactams with a Silylated Nazarov Reagent: Access to Allo and Epiallo Yohimbine-Type Derivatives.
The facial selectivity of double Michael addition reactions of the silylated Nazarov reagent 4 to unsaturated indolo[2,3-a]quinolizidine lactams 3 has been studied and the synthetic usefulness of the pentacyclic Nazarov-derived adducts is demonstrated by their conversion into alliallo yohimbine-type targets.
Tryptophanol-derived oxazolopiperidone lactams: identification of a hit compound as NMDA receptor antagonist.
Enantiopure Indolo[2,3-a]quinolizidines: Synthesis and Evaluation as NMDA Receptor Antagonists
- Nuno A. L. Pereira, F. Sureda, Maria Pérez, M. Amat, Maria M. M. Santos
- Chemistry, BiologyMolecules
- 1 August 2016
This compound represents a hit compound for the development of novel NMDA receptor antagonists with potential applications in neurodegenerative disorders associated with overactivation of NMDA receptors.
Diseño, síntesis y evaluación biológica de nuevos derivados de quinoxalina y 1,4-di-n-óxido de quinoxalina con aplicación en diferentes áreas terapéuticas
- Maria Pérez
- Chemistry, Biology
The results obtained show that the anticancer activity of the tested compounds is due to the a,â-unsaturated ketone system and that the presence of the N-oxide groups is not essential for this biological activity.