Gurdeep Singh

Breast cancer is one of the most common causes of cancer death among women in the world, and the number of tumors that depend on hormones occupies a significant percentage of cases that are diagnosed. The estrogen factor is central to the development of these cancers; hence, aromatase, the central enzyme involved in estrogen production, is a critical therapeutic target. Aromatase Inhibitors (AIs), in particular, have emerged to play an important role in endocrine therapy in postmenopausal breast cancer patients. Heterocyclic compounds, in particular, have also been receiving significant focus in the design of AI scaffolds, because they are structurally diverse and capable of binding the heme iron in the aromatase active site. This review provides extensive coverage of recent developments in heterocyclic aromatase inhibitors, including large classes such as azoles, indoles, quinolines, coumarins, benzofurans, and other fused heterocyclic systems. The focus is on trends in Structure-Activity Relationships (SAR), with emphasis on the patterns of substitution and pharmacophoric features that can modulate potency and selectivity. Mechanistic information from molecular docking and other computational studies is also presented to elucidate binding interactions and inform rational drug design. In addition, new approaches such as the development of hybrid molecules and multi-target-directed ligands are listed to illustrate emerging trends aimed at enhancing efficacy and pharmacokinetic properties. Together with heterocyclic structures, these frameworks are still offering viable and bright platforms on which next-generation aromatase inhibitors can be developed to treat breast cancer better.

Introduction: Evodiamine, a quinazoline alkaloid derived from the Evodia rutaecarpa plant, has gained significant attention owing to its promising anticancer properties. However, its clinical applications are hampered by inherent challenges, including low water solubility, poor bioavailability and potential toxicity. This study reviews the current status and the medicinal chemistry efforts to accelerate the pace of evodiamine clinical applications in cancer therapy. Methods: A comprehensive literature search in four electronic databases (PubMed, Scopus, Web of Science, Google Scholar and ScienceDirect) for this study, only English language publications have been evaluated based on their titles, abstracts and full text using keywords like evodiamine, anticancer, evodiamine derivatives, nanoformulation. Results: Structural modification and nano-delivery strategies significantly improve the pharmacokinetic profile of evodiamine, reduce toxicity, and enhance its therapeutic efficacy. These strategies provide better bioavailability, increased target specificity and improved anticancer potential. Conclusion: Integrating structural modification with nanotechnology presents a promising approach to address the challenges associated with evodiamine. This combination can potentially maximize its therapeutic efficacy in cancer treatment, paving the way for its clinical translation.

All therapeutic interventions aimed at modulating the immune response to pathogens, self‐antigens, carcinogens, or xenogeneic antigens are referred to as immunomodulation, which either prevents hyperactivation or restores the appropriate response of the immune system. Since antiquity, medicinal plants have been used as a source of immune‐boosting medicines with fewer side effects. These medicinal plants, for example, Curcuma longa , Camellia sinensis , Artemisia annua , and Andrographis paniculata , have been used to treat immune system disorders such as multiple sclerosis, psoriasis, lupus, and organ transplantation. Herein, we review the currently accessible medicinal plants, their phytoconstituents, and underlying mechanisms of immunomodulation.

Background: Diabetes mellitus and obesity are two of the most frequent health conditions in the world, prompting medical researchers to seek novel effective treatments. According to World Health Organization (WHO) regulations and several research studies, diabetes is regarded as a significant and leading health concern worldwide. The search for efficient and safe antidiabetic drugs has led to the study of pyridine derivatives, a family of molecules with a wide range of pharmacological characteristics. Pyridines are important heterocyclic chemicals renowned for their various pharmacological properties. Methods: Materials were compiled using the three databases of ScienceDirect, PubMed, and Google Scholar. For this study, only English-language publications have been evaluated based on their titles, abstracts, and full texts using keywords like diabetes, pyridine Derivatives, αglucosidase inhibitors, and α-amylase inhibitors. Results: Pyridine and its derivatives have received a lot of attention due to their wide range of potential uses in medicinal chemistry and pharmacology. Structural alterations and optimization efforts have resulted in higher effectiveness, selectivity, and safety characteristics. These discoveries highlight the importance of pyridine analogues as a novel class of therapeutic agents for diabetes management. Conclusion: The review highlights the significance of pyridine analogues in the development of antidiabetic treatments, opening new avenues for developing drugs and clinical use. The ongoing advancements in the discovery of pyridine derivatives underscore their potential as prospective agents in diabetic treatments.

Mycotoxins are toxic secondary metabolites produced by certain molds and fungi that contaminate various food commodities, posing serious adverse effects on humans and animals. Aflatoxin, ochratoxin, trichothecene, fumonisin, zearalenone, patulin, and citrinin are some of the major mycotoxins affecting food and feed. The scientific community has focused on regulating food and feed materials due to their potential risks. Conventional techniques for mycotoxin detection have certain limitations in terms of sensitivity, specificity, and speed. In recent years, nanotechnology has emerged as a promising approach to revolutionize mycotoxin detection. This review provides an overview of nanotechnology‐based detection methods for mycotoxins in food and feed, discussing the basic aspects of mycotoxins, their health hazards, and conventional methods. It also explores various nanosensors and nanodevices developed to improve the sensitivity, selectivity, and speed of mycotoxin detection, thereby enhancing food safety and security.

Background: Infections caused by parasites continue to pose a risk to both human and animal health. The most popular drug classes for treating these infections include thiabendazole, imidazothiazoles, levamisole, and avermectins (obtained from the fermentation products of Streptomyces avermitilis). The majority of bacteria that we come across in any form of infection are successfully combatted by β- lactam medicines. Similar to the majority of treatments, problems with treatment resistance to these drugs have evolved over time, necessitating the development of new anthelmintic medications. This study aims to investigate a series of quinazoline-bearing β-lactam rings as potent anthelmintic agents. Methods: The new series of quinazoline bearing β-lactam was synthesized via reaction of 5-bromo anthranilic acid with acetic anhydride to produce 6-bromo-2-methyl-4H-benzo (1,3) oxazin-4-one which was then converted into 3-amino-6-bromo-2-methylquinazolin-4(3H)-one by the reaction of hydrazine hydrate in the presence of anhydrous pyridine. The resultant intermediate then goes through a Schiff reaction with various aromatic aldehydes, followed by reflux with triethylamine and chloroacetyl chloride. Results: Structural assignments of these compounds have been made by elemental analysis, FTIR,1HNMR and Mass spectral data and the purity of the compounds was determined by TLC. Molecular docking studies showed the effective binding of synthesized derivatives with tubulin in comparison to the orientation of standard drugs. The anthelmintic activities of all the synthesized compounds were evaluated separately for their possible using common Indian earthworm Pheritima posthuma. Conclusion: A total of ten derivatives of quinazoline bearing β-lactam ring were designed, synthesized and evaluated against the Indian earthworm Pheritima posthuma. Out of ten derivatives, SQD2 and SQD6, showed promising anthelmintic activity when compared with standard drugs albendazole and piperazine citrate.

Impurities found in active pharmaceutical ingredients (APIs) and pharmaceutical products are of ever‐increasing interest. According to several regulatory agencies, purity and impurity profiles are essential. An impurity is defined as any additional inorganic or organic material, residual solvents other than the medicinal components, or undesired compounds that remain with APIs. Impurities and degradation products in bulk drug materials and pharmaceutical formulations are identified, their structures are clarified, and their quantitative determination is part of impurity profiling. Unrecognized, poisonous impurities are dangerous to health and should be identified by selective procedures to increase the safety of drug therapy, and impurity profiling has become more significant in pharmaceutical analysis. This review briefly introduces process and product‐related impurities and emphasizes the creation of cutting‐edge analytical techniques for identifying them. It discusses the use of analytical methods, particularly high‐performance thin‐layer chromatography, liquid chromatography with mass spectrometry (MS), ultrahigh‐performance liquid chromatography, gas chromatography–MS, and nuclear magnetic resonance spectroscopy for the identification of contaminants and degradation products. It has discussed the importance of the quality, efficacy, and safety of drug substances and products, including the origin, types, and quality control of impurities, the need for the development of impurity profiling methods, impurity identification, and regulatory aspects.