Letters in Drug Design & Discovery - Volume 21, Issue 6, 2024

Background: Tirzepatide (LY3298176) was approved by U.S. Food and Drug Administration (FDA) on May 13th, 2022. The drug was developed by Eli Lilly and Co. and marketed under the trade name of ‘Mounjaro’, a first-in-class ‘Twincretin’, which is a dual activator of GIP and GLP-1 receptors, resulting in improved blood sugar control in type 2 diabetics The review covered the comprehensive insight on the drug discovery journe Read More

Heterocyclic compounds are fundamental building blocks for developing novel bioactive compounds. Due to their extensive uses in both industrial and synthetic organic chemistry, quinoline and benzimidazole have recently become important heterocycles. Clinical trials have investigated quinoline and benzimidazole analogues to treat a variety of illnesses, including cancer, bacterial and fungal infection, DNA damage, etc. Read More

Background: Despite being a normal body response against invading agents, inflammation, when exaggerated, needs to be controlled to minimize damage to the body. There are several drugs in clinical use against inflammation and other inflammatory conditions. Still, side effects often limit the use of these drugs, such as gastrointestinal effects generated by COX-1 inhibitors and cardiovascular effects by COX-2 inhibitors. Thu Read More

Background: Pseudomonas aeruginosa is a common cause of nosocomial infection worldwide and is responsible for 18-61% of deaths alone. The organism has gained resistance to many known antibiotics and evolved into a multidrug-resistant strain. The LptD outer membrane protein of P. aeruginosa is a special target of interest due to its role in outer membrane biogenesis. Objective: The study aimed to gain an insight into Read More

Background: Worldwide, millions of people are affected by neurodegenerative diseases. Even though treatment may help to reduce some of the mental or physical symptoms connected with neurodegenerative diseases, there is at present no way to slow disease development and no recognized cure. Objective: The current study was carried out to explore the cholinesterase (ChE) inhibitory properties of the stem of Pi Read More

Background: Overexpressed CDK1 and CDK2 are targeted as potential sites for cancer treatment. Annona muricata fruit has been reported to have more than 100 acetogenins showing cytotoxic activities against cancer cell lines. Hence the study aims to demonstrate the cytotoxicity of ethyl acetate fruit extract, its role in cell cycle progression, and apoptosis using the MDMBA-231 breast cancer cell line. Docking, dynamics, a Read More

Objective: To explore the autophagic effect of baicalein on acute myeloid leukemia (AML) cell lines, HL-60 and THP-1, and miR-424, which regulates the baicalein effect on HL-60 and THP-1 in which autophagy was observed. Methods: The cell counting kit-8 (CCK-8) assay was used to detect the optimal concentration of baicalein in the HL-60 and THP-1 cell lines. miR-424 was detected by qPCR. The influence of baicalein on the au Read More

Background: Human estrogen receptor alpha (ERα), which is known to play a role in mediating cell proliferation, metastasis, and resistance to apoptosis, is one of the targets of breast cancer therapies. Alpha mangostin (AM) is an active xanthone compound from Garcinia mangostana L. which has activity as an ERα inhibitor. Objective: This research aims to predict the pharmacokinetic and toxicity, and to study the molec Read More

Background: Novel anti-tumor bioactivity compounds were designed by the strategy of modular hybridization with the bioactivity advantages of 5-fluorouracil and dithiocarbamate derivatives. Methods: A series of novel 5-fluorouracil-dithiocarbamate conjugates were synthesized, characterized and evaluated for their cytotoxic activities in vitro against B16, Hela and U87MG by MTT assay. Colonyformation, transwell migration, cel Read More