The DNA intercalating, ellipticine analog drug, 5,11-dimethyl-5H-indol[2,3-b]quinoline, is able to stabilize in vitro the topoisomerase II-DNA cleavable complex and to induce DNA breaks in BPV I episome in rat fibroblasts. Cytotoxicity studies with DC3F cells resistant to ellipticine strongly suggest that topoisomerase II is a cellular target involved in the mechanism of cytotoxic action of this carboline derivative.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/0006-2952(92)90341-f | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Manzamine A: A Promising Marine-Derived Cancer Therapeutic for Multi-targeted Interactions with E2F8, SIX1, AR, GSK-3β, and V-ATPase - A Systematic Review.
Eur J Pharmacol
January 2025
Department of Urology, Brown Cancer Center, 505 S Hancock Street, Louisville, KY, USA. Electronic address:
Manzamine A, a natural compound derived from various sponge genera, features a β-carboline structure and exhibits a range of biological activities, including anti-inflammatory and antimalarial effects. Its potential as an anticancer agent has been explored in several tumor models, both in vitro and in vivo, showing effects through mechanisms such as cytotoxicity, regulation of the cell cycle, inhibition of cell migration, epithelial-to-mesenchymal transition (EMT), autophagy, and apoptosis through multi-target interactions of E2F transcriptional factors, ribosomal S6 kinases, androgen receptor (AR), SIX1, GSK-3β, V-ATPase, and p53/p21/p27 cascades. This systematic review evaluates existing literature on the potential application of this marine alkaloid as a novel cancer therapy, highlighting its promising ability to inhibit cancer cell growth while causing minimal side effects.
View Article and Find Full Text PDFHFIP-mediated cascade aminomethylation and intramolecular cyclization of allenamides with ,-acetals to access tetrahydro-β-carboline derivatives.
Chem Commun (Camb)
January 2025
Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow 226031, India.
The construction of complex molecules under metal-free conditions multiple bond-forming steps in a cascade manner is highly desirable. Herein, we have developed an HFIP-alone promoted aminomethylation and intramolecular cyclization of allenamides, providing biologically relevant tetrahydro-β-carboline derivatives embedded with an allylic amine functionality. The metal-free protocol provided the desired tetrahydro-β-carboline derivatives under mild conditions.
View Article and Find Full Text PDFIdentification, Occurrence, and Mechanism of Formation of 1-Acetyl-β-carbolines Derived from l-Tryptophan and Methylglyoxal.
J Agric Food Chem
January 2025
Spanish National Research Council (CSIC), Instituto de Ciencia y Tecnología de Alimentos y Nutrición (ICTAN), Jose Antonio Nováis 6 28040, Madrid, Spain.
β-Carbolines (βCs) are bioactive compounds present in foods and biological systems. This work describes the identification, occurrence, and mechanism of formation of 1-acetyl-β-carbolines (1-acetyl-βCs) that result from the reaction of l-tryptophan with the α-dicarbonyl compound methylglyoxal. Two β-carbolines are characterized as 1-acetyl-β-carboline (AβC) and 1-acetyl-β-carboline-3-carboxylic acid (AβC-COOH).
View Article and Find Full Text PDFInteraction of normelinonine F and related N-methyl-β-carbolines derivatives with bovine serum albumin. Spectroscopic profiles, multivariate analysis and theoretical calculations.
Int J Biol Macromol
January 2025
Instituto Tecnológico de Chascomús (CONICET-UNSAM), Av. Intendente Marino Km 8.2, CC 164, B7130IWA Chascomús, Argentina; Escuela de Bio y Nanotecnologías (UNSAM), Argentina. Electronic address:
β-carbolines (βCs) represent a large family of bioactive alkaloids, including norharmane and normelinonine F, known for their diverse pharmacological activities. The effects of these alkaloids may depend, among other factors, on their delivery, accumulation in different subcellular compartments, and interactions with biomacromolecules such as serum albumins. In this study, we investigated the pH dependence of the interactions between bovine serum albumin (BSA) and four βCs (norharmane, normelinonine F, and their corresponding N(9)-methyl derivatives) using UV-vis and fluorescence spectroscopy, combined with multivariate analysis and molecular docking.
View Article and Find Full Text PDFSynthesis of harmaline N-9 derivatives and investigation of in vitro anticancer activity.
Bioorg Med Chem Lett
January 2025
School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 102488 China. Electronic address:
Harmaline as a natural compound possessed a wide range of pharmacological activities. In this study, 22 novel harmaline-based derivatives were synthesized and screened for in vitro anti-proliferation activity against three cancer cell lines, HCT116, MCF7, and MGC803. The modification site was at the position N-9 of harmaline.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!