Literature DB >> 25800433

Synthesis of novel 24-amino-25,26,27-trinorlanost-8-enes: cytotoxic and apoptotic potential in U937 cells.

Roisin O'Keeffe1, Olivia Kenny2, Nigel P Brunton3, Mohammad B Hossain4, Dilip K Rai4, Peter W Jones5, Nora O'Brien6, Anita R Maguire7, Stuart G Collins8.   

Abstract

In the present study, the synthesis of a range of novel 24-amino-25,26,27-trinorlanost-8-ene derivatives including 24-piperadino-trinorlanost-8-enes, 24-piperazino-trinorlanost-8-enes, 24-morpholino-trinorlanost-8-enes, and 24-diethylamino-trinorlanost-8-enes is reported and their cytotoxic and apoptotic potential evaluated in U937 cell lines. Excellent IC₅₀ results for piperidine and 1-(2-hydroxyethyl)piperazine derivatives have been observed (IC₅₀ values of 1.9 μM and 2.7 μM in U937 cells, respectively).
Copyright © 2015 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Apoptosis; Lanostanes; Oxidative cleavage; Reductive amination; U937 cells

Mesh:

Substances:

Year:  2015        PMID: 25800433     DOI: 10.1016/j.bmc.2015.02.034

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  2 in total

1.  Modulation of lanosterol synthase drives 24,25-epoxysterol synthesis and oligodendrocyte formation.

Authors:  Zita Hubler; Ryan M Friedrich; Joel L Sax; Dharmaraja Allimuthu; Farrah Gao; Adrianna M Rivera-León; Matthew J Pleshinger; Ilya Bederman; Drew J Adams
Journal:  Cell Chem Biol       Date:  2021-02-25       Impact factor: 9.039

2.  Trisnor-Euphane-Type Triterpenoid and Other Constituents Isolated from Euphorbia tanquahuete Sessé & Moc.: Preparation and Cytotoxic Evaluation of Semisynthetic Derivatives of Euphol.

Authors:  Luis J Romero-Morán; María Teresa Ramírez-Apan; Simón Hernández-Ortega; Diego Martínez-Otero; Guillermo Delgado
Journal:  ACS Omega       Date:  2022-09-20
  2 in total

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