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- Volume 21, Issue 11, 2024
Letters in Drug Design & Discovery - Volume 21, Issue 11, 2024
Volume 21, Issue 11, 2024
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Design of Podophyllotoxin-based Hybrid Compounds as Potential Anticancer Agents
Authors: Hezhen Wang, Xun Sun, Chunyong Wei, Jing Wang and Lei ZhangBackground: Cancer has been regarded as the leading cause of death worldwide. Identifying new anti-neoplastics with high potency and low toxicity is urgent. Objective: Podophyllotoxin-based hybrid compounds were synthesized by esterification and characterized using NMR and HR-MS. In vitro cytotoxicity and molecular mechanism studies were performed. Methods: Podophyllotoxin was hybridized with three selected known nat Read More
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Diversely Functionalized Pyridine Ring-fused Heterocycles and their Anticancer Properties
Among N-containing heterocycles, pyridine occupies a prominent position due to its presence in nature. Many enzymes in living systems, which are involved in redox reactions, contain pyridine moiety. In addition, its importance in medicinal chemistry and its presence in drugs are well documented. Several pyridine containing compounds are well-known as tubulin polymerization inhibitors and are found to bind with andr Read More
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Nanotechnology-Based Approaches for Nose-to-Brain Drug Delivery in Neurodegenerative Diseases
Drug delivery to the brain is a challenging task as many drugs do not cross the blood-brain barrier (BBB). As a result, designing strategies to target drugs to the brain requires significant effort. However, recent research has focused on the administration of drugs through the nose to the brain, a noninvasive way to bypass the BBB and deliver therapeutic molecules directly to the brain. Nose-to-brain drug delivery is a promising ap Read More
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“Thiophene”: A Sulphur Containing Heterocycle as a Privileged Scaffold
Authors: Yuthika Narayan, Ajay Kumar and Aamna ParveenIn the rapidly expanding chemical realm of heterocyclic compounds with interesting therapeutic properties, the thiophene nucleus has established itself as a prospective entity. The biological activity of comparable substances produced via different pathways is of varying magnitudes. Medicinal chemists use their understanding of multiple synthetic pathways and the various physicochemical properties of such compounds to crea Read More
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Medicinal Plants and Natural Products to Treat Obesity through Inhibiting Pancreatic Lipase: A Review (2020-2022)
Authors: Khaoula Jamai, Nour E. Daoudi, Amal Elrherabi and Mohamed BnouhamPancreatic lipase is an enzyme that catalyzes the hydrolysis of triglycerides to monoglycerides and free fatty acids which promote and accelerate their absorption by the intestine, thus leading to obesity. Drugs that have numerous side effects explain the beneficial medicinal effect of plants resulting from their Phyto molecules that exhibit strong anti-lipase activity. The present review reveals the medical treatment and conse Read More
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Implementation of PLGA-based Nanoparticles for Treatment of Colorectal Cancer
Authors: Amandeep K. Gill, Rajiv Sharma, Surya Prakash Gautam, Amanda Frank, Neha Bajwa and Preet Amol SinghColorectal cancer is more prevalent in females than males. There are many anticancer drugs accessible for use, but their therapeutic importance is constrained by factors including poor solubility, low absorption, and multi-drug resistance. This review highlights how PLGA may be used to develop polymeric- targeted drug delivery systems that specifically target colorectal cancer. The PLGA polymer, which is disseminated i Read More
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Asymmetric Dimethylarginine (ADMA) in Cardiovascular Disease, Cardiac Ischemia/reperfusion Injury, and Ischemic Non-obstructive Coronary Artery Disease: Biochemical and Pharmacological Implications
Authors: Francesco Corradi, Benedetta Bucciarelli, Francesco Bianco and Tonino BucciarelliSeveral studies have shown that high plasma concentrations of asymmetric dimethylarginine (ADMA), a known endogenous competitive inhibitor of endothelial nitric oxide synthase (eNOS), correlate with the severity of coronary artery disease (CAD), with worsening of cardiac ischemia/reperfusion (I/R) injury and coronary atherosclerosis. It is believed that it may be an important risk factor for myocardial infarc Read More
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Medicinal Plants and Bioactive Compounds with Potential Anti-inflammatory and Antidiabetic Activities: A Review
Authors: Saliha Bouknana, Amal E. Rherabi, Rhizlan Abdnim, Ali Berraaouan and Mohamed BnouhamBackground: Inflammation is a complex process. Persistent and uncontrolled inflammation may act as an etiologic factor for many chronic disorders like diabetes. Objective: This review aims to classify the anti-inflammatory and antidiabetic medicinal plants, their traditional uses, and their active compounds that have been tested for their anti-inflammatory and antidiabetic effects. Methods: We checked scientific public Read More
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Ezetimibe Inhibits Cell Viability and Invasion by Suppressing PI3K/AKT Signaling Pathway in Human Osteosarcoma Cells
Authors: Yong Zhang, Tongzhou Hu, Qiuyan Weng and Jianning LuoIntroduction: Osteosarcoma is one of the most prevalent malignant bone tumors with a poor overall prognosis and mainly happens in children and adolescents. Current therapy strategies still possess a lot of limitations, and new and efficient strategies are required. Ezetimibe was previously reported to have its anti-tumor effect in various tumors, but the investigation of Ezetimibe on osteosarcoma is still limited. Aims: This stu Read More
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Curbing Key Digestive Enzymes by Three Plant Extracts for Sustainable Management of Postprandial Hyperglycemia
Authors: Parth Sarker, Deedarul H. Sani, Md. Faruque Miah and Md. Jahangir AlamBackground: Diabetes mellitus is a chronic metabolic condition marked by persistently elevated blood sugar levels. Key digestive enzymes viz. α-amylase and α-glucosidase, hydrolyze consumed carbohydrates into glucose which raises the postprandial blood glucose level in a diabetic patient. So, the development of α-amylase and α-glucosidase inhibitors procured from medicinal plants to retard starch digestion is an alternativ Read More
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Palladium (II)-N-heterocyclic Carbene Complexes: Synthesis, Molecular Docking, UV-Vis Absorption and Enzyme Inhibition
Background: Alzheimer's disease is the most prevalent form of dementia; it affects the brain regions responsible for thought, memory, and language. Dementia cannot currently be cured by any medication. Objective: We aimed to synthesize Pd-NHC type PEPPSI and investigate their biological activity in anticholinesterase enzymes. Methods: In this study, we described preparing a series of Pd-NHC type PEPPSI obtaine Read More
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Analysis of the Safety and Effectiveness of Lenvatinib + TACE-HAIC + PD-1 Inhibitor for Intermediate and Advanced Hepatocellular Carcinoma
Authors: Yuguang Yang, Hui Tang, Cong Mai, Xin Zhang, Jiawen Kuang and Yunqiang TangBackground: Hepatocellular carcinoma (HCC) is the sixth most prevalent cancer and the fourth leading cause of cancer death in the world. Aims: This study aimed to investigate the efficacy and safety of Lenvatinib + PD-1 inhibitor + TACEHAIC (LePTaHAIC) versus Sorafenib + TACE (SorTACE) for patients with intermediate and advanced HCC. Methods: In this retrospective study, patients diagnosed with BCLC stage B/C HCC wer Read More
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Mechanism of American Ginseng Against Type 2 Diabetes Mellitus Based on Network Pharmacology & Molecular Docking
Authors: Jiaxin Li, Siqi Chen, Bo Wang, Jiaming Xie, Xinyu Wu, Xinying Hu, Jing Liu, Yi Zhang, Junzhi Wang and Pengling GeBackground: Ginseng is one of the top-selling natural products worldwide and has been shown to have significant effects. Nonetheless, there is limited research on American ginseng when compared to Asian ginseng. A small number of studies have demonstrated the therapeutic benefits of American ginseng, which include antioxidant, anti-inflammatory, and immune-stimulating activities. Objective: The objective of our rese Read More
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Novel 1,3,4-trisubstituted Pyrazolopyrimidine Derivatives Show Potent Antiproliferative Activity in Mantle Cell Lymphoma
Authors: Fansheng Ran, Lun Dong, Yang Liu and Guisen ZhaoBackground: Pyrazolopyrimidine scaffold is an important pharmacophore in drug discovery. This pharmacophore has been reported to produce numerous biological activities, of which anticancer is an important one. The development of novel pyrazolopyrimidine derivatives is of great importance for antitumor drug research. Objective: Compound 6, a pyrazolopyrimidine derivative reported by our group, showed weak Read More
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Design, Docking, Synthesis, and In vitro Evaluation of Potent Anti-tubercular Agents Targeting DNA Gyrase
Background: Tuberculosis caused by Mycobacterium tuberculosis has been reported to infect about two-third of the global population and to continuously develop multidrug resistance. DNA gyrase, a type II topoisomerase, is a promising target of the quinolone class of drugs in the treatment of tuberculosis. Objective: The present study is focused on the design and synthesis of newer nitrogen heterocyclics containin Read More
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The Implication of Fragment-centric Mapping Strategy to Explore the First Selective Inhibitor Against Target Protein
Authors: Jia-Hui Zhao, Shao-Long Zhang, Xia Zhou, Xian-Mei Meng, Ting Wang and Xie-Huang ShengIntroduction: Identification of the first selective inhibitor, also called “hit molecules, " is crucial for developing drugs against a protein target. However, the crystal structures of protein-ligand complexes are usually not resolved in time due to the process's time-consuming and costly nature. However, it does not prevent scientists from understanding the binding modes' urgent advantages and drawbacks of protein-ligand inter Read More
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A Comparative Study of Using Poly (D, L, Lactide-co-Glycolic Acid) and Chitosan Nanoparticle as Vaccine Delivery System for a Recombinant Fusion Protein of Newcastle Disease Virus
Authors: Kanagaraj Vijayarani, Sundaram Arul and Kathaperumal KumananIntroduction: The more effective method of preventing many infectious diseases is vaccination. Numerous infectious diseases that affect both humans and animals have significantly decreased as a result of routine immunization. Aim: The present study aimed to compare the efficacy of in-house built chitosan and Polylactide coglycolic acid (PLGA) nanoparticles coupled with Pichia pastoris expressed immunogenic fusion (F) Read More
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Drug Repurposing for Thioredoxin Interacting Protein Through Molecular Networking, Pharmacophore Modelling, and Molecular Docking Approaches
Authors: Ayushi Kar, Balamurugan Paramasivam, Darshini Jayakumar, Akey K. Swaroop and Jubie SelvarajBackground: Diabetes Mellitus (DM) has emerged as one of the major causes behind global all-cause mortality between the age group of 20-79 years. Thioredoxin Interacting Protein (TXNIP) is a naturally occurring protein that primarily acts by binding to TRX protein, thereby inhibiting its ability to maintain the cellular reduced environment and subsequent oxidative stress, which leads to dysfunctional insulin production and Read More
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Vitexin Induces Apoptosis and Ferroptosis and Suppresses Malignant Proliferation and Invasion of Bladder Urothelial Carcinoma through PI3K/AKT-Nrf2 Axis
Authors: Chao Wang and Huamao JiangBackground: Bladder urothelial carcinoma (BUC) is a type of malignant urinary system. Although several strategies have been applied in the treatment of BUC, its survival remains unsatisfactory, especially in the patients with advanced BUC. Vitexin, a natural flavonoid has exhibited the inhibitory effect on various tumors, however, its effect on BUC is still unclear. Objective: This study aimed to explore the effect of vitexin Read More
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Chiral Azepines: In silico Potential in Cancer and Neurodegenerative Diseases, a Chemical Analysis
Background: Chiral azepines are synthesized with remarkable diastereoselectivity, but their biological activity has not been investigated. However, benzazepines have demonstrated notable effects, particularly on the central nervous system (CNS) and infections. This characteristic attracts the interest of bioinformatic investigations in this new family, as their structural similarity can confirm their potential based on their kinship o Read More
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Volumes & issues
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Volume 21 (2024)
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Volume 20 (2023)
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Volume 19 (2022)
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Volume 18 (2021)
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Volume 17 (2020)
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Volume 16 (2019)
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Volume 15 (2018)
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Volume 14 (2017)
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Volume 13 (2016)
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Volume 12 (2015)
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Volume 11 (2014)
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Volume 10 (2013)
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Volume 9 (2012)
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Volume 8 (2011)
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Volume 7 (2010)
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Volume 6 (2009)
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Volume 5 (2008)
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Volume 4 (2007)
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Volume 3 (2006)
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Volume 2 (2005)
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Volume 1 (2004)
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