Letters in Drug Design & Discovery - Volume 20, Issue 8, 2023

Cancer-Associated Fibroblasts (CAFs) originate from the activation of fibroblasts in the Tumor Microenvironment (TME) during tumorigenesis, resulting in the promotion of tumor growth, metabolism, and metastasis. Exosomes, which can locally or remotely transfer miRNAs, lncRNAs, proteins, metabolites, and other substances to other cells, have a size and range distribution of 30 to 150 nm and have been described Read More

KRAS is a highly mutated gene among cancers, especially in the lung, pancreatic and colorectal cancers (CRC). Despite extensive efforts in the past three decades, KRAS remains undruggable. But lately, inhibitors selectively binding to cysteine mutant at 12thposition (G12C) are in clinical trials as a single agent and in combination with other drugs. FDA approved LUMAKRAS (Sotorasib, AMG510) for metastatic NSCLC, while Adagrasi Read More

Background: Epilepsy is one of the most common neurological disorders. Many individuals continue to have seizures despite medical and surgical treatments, suggesting that the discovery of novel anti-seizure drugs is vital. Triazole compounds are widely used as pharmaceuticals and have gained significant interest in medicinal chemistry. In this article, the development of triazoles, especially 1,2,4- triazole, in the field of ant Read More

Herbal medicine and phytochemicals have always been great therapeutic options to treat various diseases due to their compatibility, safety, easy production, low cost and side effects. However, low absorption rate, and poor bioavailability are notable challenges that have limited the use of most phytoconstituents. To address these challenges, different drug delivery methods have been proposed for generating operative carr Read More

Introduction: N-methyl-d-aspartate receptor (NMDAR) and tau protein play an important role in neuronal death due to cerebral ischemia or ischemic stroke. Unfortunately, no drug has been discovered except tissue plasminogen activator (tPA) to fight against ischemic stroke. Virtual high throughput screening to find out possibilities of bioactive molecules to target NMDAR and tau protein to treat ischemic stroke may be an Read More

Background: Tetrapyrrolic compounds, such as porphyrins and metalloporphyrins, are highly interesting for pharmaceutical chemistry designs considering their good biocompatibility and therapeutic potential. Objective: The aim of the present work was a preliminary in vitro evaluation of some unsymmetrical porphyrins and the corresponding symmetrical structures as potential candidates for the photodynamic therapy of Read More

Background: In the diabetic condition, damage to the Müller cells contributes to the pathogenesis of diabetic retinopathy. Aims: This study aimed to investigate the protective effect of Bushen Huoxue, Traditional Chinese Medicine (BHTCM), on Müller in diabetic retinopathological conditions. Methods: Primary rat retinal Müller cells (RRMC) were isolated and cultured under high glucose (50 nmol/L). The advanced glycation end Read More

Introduction: Although, several vaccines are being approved, no effective antiviral drug has been developed for COVID-19 infectious. The present investigation was aimed to increase the essential oils of Cuscuta campestris using far-red light treatment and examine the potential of crude extracts of C. campestris against selected pneumonia pathogens and COVID-19. Methods: Anti-COVID-19 activity was determined in hu Read More

Aim: The present work has been designed to discover some novel 2-substituted -5-hydroxy-1- (1-methyl-3-morpholinopropyl)-1H-indole-3-carboxamide derivatives and their screening through computational molecular docking. Background: The present manuscript describes designing novel 2-substituted-5-hydroxy-1-(1-methyl-3- morpholinopropyl)-1H-indole-3-carboxamide derivatives as specific ERα modulators, discus Read More

Background: Staphylococcus aureus (S. aureus) is a Gram-positive bacterium causing a wide range of human infections, leading to life-threatening invasive disorders, hospitalization, and mortality. Producing β-lactamase enzymes in S. aureus is one of the main mechanisms of the pathogen that makes the bacteria resistant to beta-lactam antibiotics, resulting in methicillin-resistant S. aureus (MRSA) strains. Therefore, it is crucial t Read More

Introduction: 2-Amino-7-hydroxy-4-phenyl-4H-chromene-3-carbonitrile (4) was synthesized through a three-component reaction in ethanol/piperidine solution. Methods: Synthesis of several new 4H-chromenes (5-14) has been achieved involving various reactions. The structure of these new compounds was confirmed using IR, 1H NMR and 13C NMR, as well as MS spectroscopy. Results and Conclusion: All newly sub Read More

Background: Anticipating the correlation between SARS-CoV-2 infection and ‘triplenegative breast cancer (TNBC)’ remains challenging. It has been reported that people currently diagnosed with cancer have a higher risk of severe complications if they are affected by the viral infection. Cancer treatments, including chemotherapy, targeted therapies, and immunotherapy, may weaken the immune system and possibly cause criti Read More

Objectives: Glutamatergic dysfunction has been implicated in the pathogenesis of numerous central nervous system disorders. Artemisia absinthium (A. absinthium), has been reported to have neuroprotective and antioxidant activities. The current study examined the effect of A. absinthium extract on glutamate-induced cytotoxicity using PC12 cells. Methods: PC12 cells were pretreated with A. absinthium extract ( Read More

Background: Osteosarcoma (OS) is the most prevalent primary bone sarcoma in the global child and young adult population, and the current mainstream treatment regimens are not very effective. The unique efficacy of traditional Chinese medicine (TCM) for cancers has recently received increasing attention. Oldenlandia diffusa (OD) is commonly used as adjuvant therapy for various cancers in Chinese herb medicine (CHM Read More

Background: Most of the structural modifications to evodiamine (EVO) have focused on the 3- and 10-positions, while structural modifications to the EVO 2-position have not yet been reported. In this study, we investigated the scaffold diversity and bioactivity of EVO from position 2 to gain more insight into the influence of the chemical space around EVO on bioactivity. Objective: The study aims to synthesize two derivatives of EV Read More

Background: Rapidly dissolving oral strips have many advantages, especially in pediatric and geriatric use. Benzydamine hydrochloride is an active substance with local analgesic, anesthetic, antimicrobial and non-steroidal anti-inflammatory properties. Objective: The aim of the study was to formulate and characterize orally dispersible benzydamine hydrochloride- loaded fast dissolving oral strips for the sufficient treatment o Read More

Background: Angiogenesis is a natural and complex mechanism that is regulated by biomolecules formed by the body. Medicinal inorganic chemistry is increasing in popularity due to metal-based compounds, offering significant chances and possibilities for building novel anti-cancer medicines with promising anti-angiogenic effects. Objective: This study aimed to examine the successful results obtained from treatmen Read More