Category Ranking
98%
Total Visits
921
Avg Visit Duration
2 minutes
Citations
20
Article Abstract
A number of new 1-substituted-6H-pyrido[4,3-b]carbazole derivatives have been synthesized. Nine of the newly obtained compounds were subjected to preliminary in vitro cytostatic activity screening against murine leukemia (L1210), human lung cancer (A549) and human colon cancer (HT29) cell lines. One particular compound 6f exhibited over 20 times better activity against L1210 tumor cell line than the reference ellipticine.
Download full-text PDF |
Source |
|---|
Publication Analysis
Top Keywords
Similar Publications
Platinum-group metal half-sandwich complexes of sugar-isoxazol(in)e conjugates - synthesis and evaluation of their antineoplastic and antimicrobial activities.
Eur J Pharm Sci
September 2025
Department of Organic Chemistry, University of Debrecen, P.O. Box 400, H-4002 Debrecen, Hungary. Electronic address:
Platinum-group metal half-sandwich complexes are considered to be potential replacements of the clinically widely used platins which have several side effects and tend to cause resistance to develop. In our previous works, we used a range of 2-pyridyl-substituted N- and C-glycosyl heterocycles as N,N-chelating ligands to prepare ruthenium(II), osmium(II), iridium(III) and rhodium(III) polyhapto arene/arenyl half-sandwich complexes. Some of these complexes, particularly with the C-glucopyranosyl isoxazole derived ligand in its O-perbenzoylated form, exhibited greater anticancer efficiency than cisplatin and had minimal or negligible effects on non-transformed fibroblasts.
View Article and Find Full Text PDFThe Development of -Methyl-BODIPY Conjugates with Boc--CBI and Cabozantinib: The Practical Challenges of Red-Light-Activated Prodrugs for Anticancer PDT.
Bioconjug Chem
September 2025
Lobachevsky State University of Nizhny Novgorod, Gagarina av. 23, Nizhny Novgorod 603950, Russian Federation.
Latest studies highlight boron-dipyrromethene (BODIPY) with a -methyl moiety as a promising photoremovable protecting group due to its activation within the phototherapeutic window. While BODIPYs inherently generate ROS and act as photosensitizers, few studies have explored combining their photouncaging capability with photodynamic therapy (PDT). Herein, we developed novel -methyl-BODIPY conjugates of the DNA alkylator Boc--CBI and the multikinase inhibitor cabozantinib derivative activated by green or red light.
View Article and Find Full Text PDFThe HDAC inhibitor romidepsin renders liver cancer vulnerable to RTK targeting and immunologically active.
Nat Commun
August 2025
Aix Marseille Univ, CNRS, Inserm, Institut Paoli-Calmettes, Centre de Recherche en Cancérologie de Marseille (CRCM), Marseille, France.
Histone deacetylases (HDACs) are epigenetic regulators frequently altered in cancer. Here we report that overexpression of HDAC1/2 occurs in Hepatocellular Carcinoma (HCC) patients, correlating with poor prognosis. We show that romidepsin, a class-I HDAC inhibitor, elicits a combinatorial perturbation of distinct molecular processes in HCC cells, altering lipid composition, mitotic spindle machinery, and levels of cell cycle/survival signals.
View Article and Find Full Text PDFHit-to-Lead Studies of Pyrazinylpiperazines against Visceral Leishmaniasis: Pharmacokinetic Profile and Efficacy of Potent Compounds against .
ACS Pharmacol Transl Sci
August 2025
Laboratório de Síntese de Candidatos a Fármacos, Instituto de Química, Universidade Federal de Uberlândia (UFU), Uberlândia, MG 38400-902, Brazil.
As part of the hit-to-lead optimization of antileishmanial pyrazinylpiperazines, the Absorption, Distribution, Metabolism, and Excretion (ADME) properties of the initial hit and five candidates for studies were assessed . These candidates, which displayed improved potency against (IC < 5 μM), were selected from an earlier structure-activity relationship study. Such assessment revealed that, except for the catechol derivative , all derivatives exhibited an improved overall ADME profile in comparison to the initial hit.
View Article and Find Full Text PDFAnticancer Activity of the Marine-Derived Compound Bryostatin 1: Preclinical and Clinical Evaluation.
Int J Mol Sci
August 2025
Department of Medical Biology, Medical University of Lodz, Muszynskiego 1, 90-151 Lodz, Poland.
Bryostatin 1, a natural macrolide isolated from , is a potent modulator of protein kinase C (PKC) isoforms with promising anticancer properties. In numerous in vitro studies, bryostatin 1 has been shown to inhibit tumor cell proliferation and induce differentiation and apoptotic cell death in a wide range of cell lines, including leukemia, lymphoma, glioma, and solid tumors such as ovarian and breast cancer. Its antitumor activity, both as monotherapy and in combination with conventional chemotherapy, has been confirmed in in vivo models, where synergistic effects have been observed, including sensitization of tumor cells to cytostatic agents.
View Article and Find Full Text PDF