The antineoplastic properties of alpha-carboline, alpha-carboline hydrochloride, alpha-carboline N-1 methyl iodide and c-6 substituted fluoro-, chloro, nitro- and phenyl-alpha-carboline were studied. None of the compounds proved to be active when tested against i.p. transplanted B16 melanoma or i.m. implanted Lewis lung carcinoma. In addition, alpha-carboline was assessed against i.p. inoculated plasmacytoma MP26 and colon carcinoma 26, and solid tumors of mammary carcinoma 16/C and Walker carcinosarcoma 256. Under conditions tested these neoplasms did not respond to alpha-carboline.
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Eur J Med Chem
October 2024
Université Paris-Saclay, CNRS, BioCIS, 94400, Orsay, France. Electronic address:
J Org Chem
July 2023
School of Chemistry and Chemical Engineering, Key Laboratory of Surface & Interface Science of Polymer Materials of Zhejiang Province, Zhejiang Sci-Tech University, Hangzhou 310018, China.
Bioorg Chem
April 2023
School of Life Science and Technology, Weifang Medical University, Shandong, China. Electronic address:
A series of new α-carboline analogues modified at N or N positions by alkyl, benzyl and phenyl were synthesized and characterized as potential ligands for AD therapy. These compounds exhibited multifunctional neurobiological activities including anti-neuroinflammatory, neuroprotective and cholinesterase inhibition. Among them, compound 5d with good drug-like properties and no cytotoxicity, showed potent inhibitory activity against NO production (IC = 1.
View Article and Find Full Text PDFFront Chem
August 2022
Department of Pharmacy, First Affiliated Hospital of Gannan Medical University, Ganzhou, China.
α-carboline (9-pyrido[2,3-]indole), contains a pyridine ring fused with an indole backbone, is a promising scaffold for medicinal chemistry. In recent decades, accumulating evidence shows that α-carboline natural products and their derivatives possess diverse bioactivities. However, hitherto, there is no comprehensive review to systematically summarize this important class of alkaloids.
View Article and Find Full Text PDFEur J Med Chem
October 2022
Department of Pharmaceutical/Medicinal Chemistry, Eberhard Karls Universität Tübingen, Auf der Morgenstelle 8, 72076, Tübingen, DE, Germany; Cluster of Excellence 'Image Guided and Functionally Instructed Tumor Therapies' (iFIT), Eberhard Karls University of Tübingen, 72076, Tübingen, Germany; German Consortium for Translational Cancer Research (DKTK), Partner Site Tübingen, German Cancer Research Center (DKFZ), 69120, Heidelberg, Germany; Tuebingen Center for Academic Drug Discovery, Auf der Morgenstelle 8, 72076, Tübingen, DE, Germany. Electronic address:
The mitogen-activated protein kinase kinase 4 (MKK4) has recently been identified as druggable target for the treatment of acute liver failure in RNAi experiments. In these experiments MKK4 was identified to be a major regulator in hepatocyte regeneration. Inhibitors thereof may serve as medication to promote liver regeneration or reducing hepatocyte death.
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