Asif Husain

Benzofuran, an oxygen-containing fused heterocyclic aromatic compound, occurs naturally as a secondary metabolite from various plant sources like Rutaceae, Asteraceae, Cyperaceae, and Liliaceae. The derivatives of benzofuran possess a wide range of biological activities, including anticancer, anti-inflammatory, antioxidant, antibiotic, analgesic, anti-Alzheimer’s, and immunosuppressive effects. Various synthetic methods are currently used to prepare various benzofuran derivatives. Its therapeutic significance is highlighted by the presence of the benzofuran core in several FDA-approved drugs. Due to the development of resistance in existing anticancer therapies, there is an urgent need for novel, effective, and safe therapeutic approaches. Many heterocyclic moieties and their structural hybrids have been explored for their potential biological activity and have attracted considerable attention as anticancer agents. Substituted benzofuran derivatives are emerging as lead candidates to meet the global challenges of cancer and its available treatment. Benzofuran has the chemical formula C8H6O. Structurally, it consists of a fused ring system: a benzene ring fused to a five-membered furan ring (with one oxygen). Both benzene and furan contribute to its aromatic character. Benzofuran heterocycle plays an important role in drug design and drug discovery due to its versatile nature. The current review summarizes the recent progress in the design, development, drug discovery, and pharmacological actions of benzofuran derivatives as anticancer agents; their molecular docking studies; and structure-activity relationships reported over the past five to six years, emphasizing fused heterocyclic analogues and their prospects to develop as lead molecules. A thorough understanding of the structure-activity relationship will provide a valuable framework for novel drug discovery and design.

Remibrutinib (Rhapsido^®), is an innovative oral Bruton's tyrosine kinase (BTK) inhibitor discovered and developed by Novartis for the treatment of chronic spontaneous urticaria (CSU), an autoimmune disease. It is a covalent, irreversible inhibitor that targets BTK, a key signalling node in the FcεRI pathway of mast cells and basophils, thereby suppressing the release of histamine and other inflammatory mediators. In September 2025, remibrutinib received its first US FDA approval for the treatment of CSU for adult patients who remain symptomatic despite H1 antihistamine treatment. This approval marks a significant advancement in CSU care that targets mast cell and basophil activation, two key contributors involved in hive formation and itching. This article reviews the development journey, scientific rationale, chemistry, pharmacological properties (pharmacokinetic, pharmacodynamics and safety profile), clinical trials, and granted patents that led to first FDA approval of an oral treatment for adult patients with CSU.

The emerging potential of senotherapeutics in the management of chronic pulmonary diseases focuses on the pivotal role of cellular senescence in the pathogenesis of conditions such as idiopathic pulmonary fibrosis (IPF), asthma, and chronic obstructive pulmonary disease (COPD). Senescent cells, characterized by irreversible cell cycle arrest and a pro-inflammatory secretory phenotype, accumulate with age and contribute to chronic inflammation, tissue remodeling, and disease progression in the lungs. The chapter provides an in-depth understanding of the mechanisms by which senescent cells influence pulmonary pathology and presents senolytics and senomorphics as innovative therapeutic strategies. These approaches aim to either eliminate or modulate the effects of senescent cells. While challenges such as adverse drug reactions remain, recent advancements—such as the development of FOXO4-DRI, a senolytic peptide—highlight the therapeutic promise of senotherapy in improving lung function and reducing disease burden. Ultimately, targeting senescent cells offers a dual benefit: alleviating symptoms and addressing the root causes of chronic lung disorders.

The triptans class of pharmaceuticals, which was created to treat acute migraine, is made up of indole-containing drugs that bind to a subset (1B/1D) of 5-hydroxytryptamine receptors and are agonists of serotonin receptors. At the moment, naratriptan, eletriptan, zolmitriptan, rizatriptan, almotriptan, and frovatriptan are the seven types of triptans available on the market. Among these are the FDA-approved triptans, Zolmitriptan and Sumatriptan, which are selective serotonin (5-hydroxytryptamine) agonists. Zolmitriptan, a synthetic tryptamine derivative and a well-known member of the triptan family, is available as an orally disintegrating tablet, nasal spray, and tablet. There are melt formulations of rizatriptan and zolmitriptan available on the market that are easier to use and absorb, comparable to regular pills. Recently, the FDA approved zolmitriptan, a medication with tolerability comparable to sumatriptan. Whereas zolmitriptan is only available as an oral melt or tablet, sumatriptan is available as a nasal spray, oral preparation, or self-injectable kit. The only known antimigraine drugs that were widely utilized before the triptan period were ergotamine and dihydroergotamine. However, zolmitriptan binds to plasma proteins only 25% of the time because of significant first-pass degradation. Researchers have looked into fresh ideas for solving this issue and innovations to overcome its pharmacokinetic difficulties. This article emphasizes the role of zolmitriptan in the treatment of migraines, highlighting its pharmacological properties, production, metabolism, and structural features.

Ebola virus disease (EVD) is a rare, highly contagious and a deadly disease with a variable fatality rate ranging from 30% to 90%. Over the past two decades, Ebola pandemic has severely affected the sub-Sahara region including Democratic Republic of the Congo (DRC), and Uganda. The causative agents of the most EVD cases are three distinct species out of six Ebolaviruses namely Zaire Ebolavirus (ZEBOV), Sudan Ebolavirus (SUDV) and Bundibugyo Ebolavirus (BDBV). In recent years, significant strides have been made in therapeutic interventions. Notably, the US Food and Drug Administration has approved two monoclonal antibodies: Inmazeb^TM (REGN-EB3) and Ansuvimab or Ebanga™. Additionally, many small molecules are currently in the developmental stage, promising further progress in medical treatment. Addressing the critical need for preventive measures, this review provides an in-depth analysis of the licensed Ebola vaccines-Ervebo and the combination of Zabdeno (Ad26.ZEBOV) and Mvabea (MVA-BN-Filo) as well as the vaccines which are currently being tested for their efficacy and safety in clinical studies. These vaccines might play an important role in curbing the spread and mitigating the impact of this lethal disease. The current treatment landscape for EVD encompasses both nutritional (supportive) and drug therapies. The review comprehensively details the origin, pathogenesis, and epidemiology of EVD, shedding light on the ongoing efforts to combat this devastating disease. It explores small molecules in various stages of the development, discusses patents filed or granted, and delves into the clinical and supportive therapies that form the cornerstone of EVD management. This review aims to provide the recent developments made in the design and synthesis of small molecules for scientific community to facilitate a deeper understanding of the disease and fostering the development of effective strategies for prevention, treatment, and control of EVD.

One of the triazole tautomers, 1,2,4‐triazole derivatives, has a wide range of biological activities that suggest its potential therapeutic utility in medicinal chemistry. These actions include anti‐inflammatory, anti‐cancer, anti‐bacterial, anti‐tuberculosis, and anti‐diabetic effects. Using computational simulations and models, we investigate the structure‐activity relationships of 1,2,4‐triazoles, showing how various modifications to the triazole core yield a variety of clinical therapeutic benefits. The review highlights the anti‐inflammatory effect of 1,2,4‐triazoles in relation to their ability to disrupt significant inflammatory mediators and pathways. We present in‐silico data that illuminate the triazoles′ capacity to inhibit cell division, encourage apoptosis, and stop metastasis in a range of cancer models. This review looks at the bactericidal and bacteriostatic properties of 1,2,4‐triazole derivatives, with a focus on their potential efficacy against multi‐drug resistant bacterial infections and their usage in tuberculosis therapy. In order to better understand these substances′ potential anti‐diabetic benefits, this review also looks at how they affect glucose metabolism regulation and insulin responsiveness. Coordinated efforts are required to translate the efficacy of 1,2,4‐triazole compounds in preclinical models into practical therapeutic benefits. Based on the information provided, it can be concluded that 1,2,4‐triazole derivatives are a promising class of diverse therapeutic agents with potential utility in a range of disorders. Their development and improvement might herald a new era of medical care that will be immensely advantageous to both patients and the medical community as a whole. This comprehensive research, which is further reinforced by in‐silico investigations, highlights the great medicinal potential of 1,2,4‐triazoles. Additionally, this study encourages more research into these substances and their enhancement for use in pharmaceutical development.

Benzoxazine and quinazoline are nitrogen-containing heterocyclic scaffolds found in various biologically active compounds. Due to their diverse biological actions, these heterocyclic rings serve as crucial frameworks for designing medicinal compounds. This study aimed to synthesize and assess in vivo anti-inflammatory, analgesic, and low ulcerogenic potential of a few novel benz[d][1,3]-oxazin-4-one and quinazolinone derivatives. Benzoxazinones (3a-e) were synthesized by cyclizing the carboxylic group (-COOH) of five nonsteroidal anti-inflammatory drugs viz., aceclofenac, ibuprofen, diclofenac, mefenamic acid and ketoprofen (2a-e) with anthranilic acid (1) using dry phosphorus oxychloride (POCl3) in pyridine. The corresponding quinazolinone derivatives (5a-e) were obtained by reacting 3a-e with isonicotinic acid hydrazide (4). Both sets of compounds were evaluated for their anti-inflammatory, analgesic effects, and ulcerogenicity in animal models. Structural characterization was performed using spectral analysis. Among the benzoxazinone derivatives, compound 2-(2-((2,6-dichlorophenyl) amino) benzyl)-4H-benzo[d][1,3]oxazin-4-one (3d) exhibited significant anti-inflammatory activity (62.61% inhibition of rat paw edema) and analgesic activity (62.36% protection in acetic acid-induced writhings) with tolerable gastrointestinal toxicity (2.67 ulcerogenicity index) compared to quinazolinone derivatives. The results of anti-inflammatory and analgesic activities of both the series are comparable with the respective, positive control. Compound 3d, a benzoxazinone-diclofenac hybrid, emerged as a lead molecule with potent anti-inflammatory, analgesic activities and moderate gastric toxicity showcasing the promising potential for further development.

Cancer has become a major concern in healthcare globally, and over time, incidences and prevalence of cancer are increasing. To counter this, a lot of anticancer drugs are approved and are in clinical use, playing a pivotal role in its treatment. Due to drug resistance and adverse effects, a continuous demand for novel, potent, and safe candidates to treat cancer is always there. Over the last few decades, various heterocyclic ring‐based derivatives have been explored and reported in the literature. In this regard, benzothiazole scaffold‐based compound emerged as the versatile ring for developing novel and safe anticancer candidates. In this article, we have reported various benzothiazole heterocyclic ring‐based derivatives demonstrating potent antiproliferative activity by induction of apoptosis via an intrinsic pathway in a dose‐dependent manner. These compounds also displayed inhibition of different enzymes, for example, Aurora kinase, epidermal growth factor receptor, vascular endothelial growth factor receptor, phosphoinositide kinases, DNA topoisomerase, and tubulin polymerases. This study focused on a comprehensive overview of antiproliferative activity, structure–activity relationship, apoptosis induction activity, and enzyme inhibition by benzothiazole‐based compounds.

In order to determine whether thiazolobenzamide molecules connected to naphthalene could inhibit the growth of three different tumor cell lines, MCF7 (breast carcinoma), A549 (pulmonary carcinoma), and DU145 (prostatic adenocarcinoma) a novel series of ten molecules, designated TA 1‐10, was designed, synthesized, and tested. Among these compounds, TA7 showed promising results against cell lines, especially showing exceptional efficacy against breast cancer. Antioxidant activity tests consistently showed the best performance from the TA7 molecule. Furthermore, when a dose of 50 to 500 mg/kg of the total mass of rats is given, the most effective chemical, TA7, did not exhibit any harmful effects during acute oral toxicity tests. The biochemical indicators (SGOT and SGPT) for hepatotoxicity associated with compound TA7 were found to be fairly similar to those of the control group. The findings from molecular docking, XP visualization, and MM‐GBSA dG binding investigations are in agreement with the outcomes of in‐vitro tests of antioxidant and anticancer capabilities. TA7 was the most effective compound among those that were docked; it bound free energy and had adequate properties for metabolism (biochemical processes), distribution (dispersion), absorption (assimilation), and excretion (elimination). This study found that the TA7 molecule, a thiazole ring system derivative connected to naphthalene, is to be a promising and possible anticancer agent and its efficacy may be further explored in clinical studies.

This article emphasizes the importance of prodrugs and their diverse spectrum of effects in the field of developing novel drugs for a variety of biological applications. Prodrugs are chemicals that are supplied inactively, but then go through enzymatic and chemical transformation in vivo to release the active parent medication that can have the desired pharmacological effect. By adding an inactive chemical moiety, prodrugs are improved in a number of ways that contribute to their potency and durability. For the purpose of illustrating the usefulness of the prodrug approach, this review covers examples of prodrugs that have been made available or are now undergoing human trials. Additionally, it included lists of the most common functional groups, carrier linkers, and reactive chemicals that can be used to create prodrugs. The current study also provides a brief introduction, several chemical methods and modifications for creating prodrugs and mutual prodrugs, as well as an explanation of recent advancements and difficulties in the field of prodrug design. The primary chemical carriers employed in the creation of prodrugs, such as esters, amides, imides, NH‐acidic carriers, amines, alcohols, carbonyl, carboxylic, and azo‐linkages, are also discussed. This review also discusses glycosidic and triglyceride mutually activated prodrugs, which aim to deliver the drugs after bioconversion at the intended site of action. The article also discusses the extensive chemistry and wide variety of applications of recently approved prodrugs, such as antibacterial, anti‐inflammatory, cardiovascular, antiplatelet, antihypertensive, atherosclerotic, antiviral, etc. In order to illustrate the prodrug and mutual drug concept's various applications and highlight its many triumphs in overcoming the formulation and delivery of problematic pharmaceuticals, this work represents a thorough guide that includes the synthetic moiety for the reader.