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A Review of the Medicinal Importance and Perspectives of the 2-isoxazoline Scaffold
Authors: Shilpi Pathak, Pooja Singh and Gaurav JadonAvailable online: 28 October 2024More LessThe 2-isoxazoline scaffold has emerged as a key structure in medicinal chemistry, with great therapeutic potential for a wide range of biological targets. This review investigates the medicinal value of the 2-isoxazoline scaffold, emphasizing its adaptability and usefulness in the development of new medications. Isoxazoline has a wide range of biological actions, including antibacterial, anti-inflammatory, anticancer, and anti-para Read More
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Arylcarboxamide Derivatives as Promising HDAC8 Inhibitors: An Overview in Light of Structure-activity Relationship and Binding Mode of Interaction Analysis
Authors: Suvankar Banerjee, Sandip Kumar Baidya, Tarun Jha, Balaram Ghosh and Nilanjan AdhikariAvailable online: 24 October 2024More LessHDAC8 is associated with several disease conditions as well as various cancers of several organs and hematological malignancies. To counter such pathophysiological and disease conditions, inhibition of HDAC8 may be a promising approach for anticancer drug development. In this article, a detail of arylcarboxamide-based potential HDAC8 inhibitors has been outlined. Considering their binding pattern of interactions along wit Read More
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In silico Study of Novel Tryptanthrin-Based Topoisomerase Inhibitors
Authors: Mukesh Kumar Kumawat and Kapil KumarAvailable online: 24 October 2024More LessBackground Over the past ten years, a remarkable number of changes have occurred in the field of cancer drug research. Most anticancer drugs from the first generation work by breaking down DNA, preventing its production, interfering with cell division processes, or attaching to microtubules. The potential use of tryptanthrin as well as its analogues is well documented for anticancer properties. Objective To design Read More
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Heterocyclic Compounds as Bcr-Abl Tyrosine Kinase Inhibitors Against Chronic Myeloid Leukemia
Authors: Sarah Gado, Mohammed Al-Kassim Hassan, Mehmet Murat Kisla and Zeynep Ates-AlagozAvailable online: 11 October 2024More LessDespite significant progress in oncology therapeutics, cancer remains a leading cause of mortality worldwide. Chronic myeloid leukemia, which accounts for 15% of all adult leukemia cases, is characterized by chromosomal abnormalities involving the fusion of the Bcr and Abl genes to form the Bcr-Abl oncogene. Current drug treatment of the disease involves the use of Bcr-Abl tyrosine kinase inhibitors belonging to the first, Read More
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De novo Drug Design and Repurposing to suppress Liver Cancer via VEGF-R1 Mechanism: Comprehensive Molecular Docking, Molecular Dynamics Simulations and ADME Estimation
By Soykan AgarAvailable online: 11 October 2024More LessAims The aim is to halt the progression of liver cancer [Hepatocellular carcinoma] by suppressing the VEGF-R1 receptor using Myricetin and its de novo-designed analogues. Background VEGF/VEGFR autocrine signalling promotes the growth, progression, and metastasis of Hepatocellular carcinoma, making the development of molecularly targeted therapies highly feasible. Invasive and metastatic behaviours in various ca Read More
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Design and Development of [1,2,4]Triazolo[4,3-b][1,2,4]triazines as Potential Anticancer Agents with Genotoxicity and Apoptotic Activity
Available online: 09 October 2024More LessAims: In this current study, a new series of triazolo-triazine derivatives were designed and synthesized as potential anticancer agents. Methods: The antiproliferative activity of the new compounds was evaluated against three different cancerous cell lines (MDA-MB-231, HCT-116, A549, and HT-29) using an MTT assay. To evaluate the mechanism of action, the ability of the best compound in apoptosis induction and DNA damage was Read More
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