Medicinal Chemistry

Breast cancer affects large number of women and the incidence of its occurrence is increasing annually. Human estrogen receptor alpha over expression known as one of the causes of breast cancer. Naturally produced medicinal compounds are well known for their efficacy and safety. In this study the focus is on two naturally occurring compounds which are found to have antitumor activities and they are found in a plant that has been used traditionally for breast cancer treatment for long time. These two compounds are Lapachol and 2-(1-hydroxyethyl)-naphtho[2,3-b] furan-4,9-dione, Fulvestrant was used as a control. swissDock was used for docking of the three compounds against Human Estrogen Receptor alpha and then they were evaluated for their dug likeness properties. Lapachol and 2-(1-hydroxyethyl)-naphtho[2,3-b] furan-4,9-dione showed slightly lower binding energy and better drug likeness properties than the standard. Showing that they can be farther investigated as oral anti Human Estrogen Receptor alpha agents.

In recent studies on cancer treatment, researchers find out that several enzymatic mutations lead to the development of cancerous cells. Such as Indoleamine 2,3-dioxygenase 1 (IDO1), B-Raf kinase, and ErB4 (HER4) kinase inhibitors. Imidazothiazole-based derivatives are gained more attention among scientists due to their wide variety of pharmacological activities, such as anti-fungal, anti-bacterial, anthelmintic, and anti-cancer activities as well as ease of synthesis of these compounds. During the search for compounds that can act as anti-neoplastic agents through inhibition of these enzymatic receptors, researchers found that imidazothiazole-based compounds and their derivatives show more potent anticancer activity. In this review, we focus on some traditional synthetic methods proposed by researchers to prepare imidazothiazole derivatives and their anticancer potential along with docking studies and cell line studies. Which will help researchers to develop their studies through imidazothiazole derivatives.

Antibiotics were one of the most significant discoveries of the twentieth century, saving millions of lives from infectious diseases. Because of the high selection pressure from increasing use and misuse of antibiotics over the years, microbes have developed acquired antimicrobial resistance to many drugs. AMR is primarily transmitted and acquired through human-to-human contact both inside and outside of healthcare facilities. A wide range of interconnected factors related to healthcare and agriculture govern the spread of AMR via various drug-resistance mechanisms. The unrestricted use of antimicrobials in livestock feed has been a major contributor to the emergence and spread of AMR. The prevalence of antimicrobial-resistant bacteria has reached an unprecedented level worldwide, posing a silent pandemic threat to global public health and necessitating immediate intervention.

Cancer is a broad group of diseases that can affect any organ or tissue in the body due to abnormal cellular growth for unknown reasons. Many existing chemotherapeutic agents are highly toxic and have low selectivity. They also contribute to the development of therapeutic resistance. As a result, cancer treatment requires the development of targeted chemotherapeutic agents with low side effects and high selectivity. Quinazoline is a critical scaffold that has been linked to a variety of biological activities. One of the most notable biological activities of this scaffold is its anticancer activity. Several established anticancer quinazolines work on various molecular targets via different mechanisms. The goal of this review is to present various aspects of medicinal chemistry such as drug design, structure-activity relationship, and mode of action of some anticancer quinazoline derivatives. It focuses on the chemotherapeutic activity of quinazolines from the standpoint of drug discovery and development. This review provides medicinal chemists with a bird's-eye view to aid in their efforts to design and synthesise novel quinazolines as targeted chemotherapeutic agents.

Drug screening is a crucial process used to detect the presence of drugs or their metabolites in biological samples to identify substance abuse, monitor therapeutic drug levels, and ensure safety in various settings, including workplaces, sports, and healthcare. The history of drug screening dates back to the early 20th century when rudimentary methods were employed. However, with advances in technology and understanding of drug metabolism, drug screening has evolved significantly, providing more accurate and efficient results. This article aims to delve into the principles, methodologies, applications, challenges, and future prospects of drug screening. Drug screening relies on the principles of analytical chemistry and pharmacokinetics. The process involves collecting biological samples, such as urine, blood, hair, saliva, or sweat, from individuals and subjecting them to various testing techniques. These techniques aim to identify the presence of specific drugs, their metabolites, or biomarkers that indicate drug use. Immunoassays, Gas Chromatography-Mass Spectrometry (GC-MS), Liquid Chromatography-Mass Spectrometry (LC-MS), and Enzyme-Linked Immunosorbent Assays (ELISA) are some of the widely used methods for drug screening.