Mini Reviews in Medicinal Chemistry - Volume 22, Issue 4, 2022

Recent studies have shown a significant growth of skin cancer cases in northern regions of the world, in which its presence was not common. Skin cancer is one of the cancers that mostly affects the world’s population, ranking fifth in studies conducted in the United States (USA). Melanoma is cancer that has the highest number of deaths worldwide since it is the most resistant skin cancer to current treatments. This is why alternatives for its treatment has been investigated considering nanomedicine concepts. This study approaches the role of this field in the creation of promising electrospun devices, composed of nanoparticles and nanofibers, among other structures, capable of directing and/or loading active drugs and/or materials with the objective of inhibiting the growth of melanoma cells or even eliminating those cells.

This mini review will give an insight into the need and usefulness of investigating the solubilization of poorly soluble drugs. Commonly used experimental and theoretical models are outlined to study the efficacy of the carrier or excipient for the poorly soluble drugs. Furthermore, the use of surface active agents for drug solubilization is discussed in correlation with the mathematical models suggested from time to time. A few experimental techniques are also discussed which would be very helpful in elucidating the interactions prevailing in the mixed systems of poorly soluble drugs and surface active agents.

Background: Type 2 diabetes mellitus (T2DM) is one of the most serious and prevalent diseases worldwide. In the last decade, type 2 sodium-glucose cotransporter inhibitors (iSGLT2) were approved as alternative drugs for the pharmacological treatment of T2DM. The anti-hyperglycemic mechanism of action of these drugs involves glycosuria. In addition, SGLT2 inhibitors cause beneficial effects such as weight loss, a decrease in blood pressure, and others. Objective: This review aimed to describe the origin of SGLT2 inhibitors and analyze their recent development in preclinical and clinical trials. Results: In 2013, the FDA approved SGLT2 inhibitors as a new alternative for the treatment of T2DM. These drugs have shown good tolerance with few adverse effects in clinical trials. Additionally, new potential anti-T2DM agents based on iSGLT2 (O-, C-, and N-glucosides) have exhibited a favorable profile in preclinical evaluations, making them candidates for advanced clinical trials. Conclusion: The clinical results of SGLT2 inhibitors show the importance of this drug class as new anti-T2DM agents with a potential dual effect. Additionally, the preclinical results of SGLT2 inhibitors favor the design and development of more selective new agents. However, several adverse effects could be a potential risk for patients.

Oleanolic acid (OA) is a pentacyclic triterpenoid class of natural products that possess a broad range of biological activities, specifically anticancer activities. Considering the anticancer potential of OA, a large number of analogs have been prepared by several researchers through modifications at C-3, C-12, and C-28 -COOH to develop potent anticancer agents with improved cytotoxicity and pharmaceutical properties. Some of the synthesized derivatives have been assessed in clinical trials also. This review summarizes the most recent synthetic and biological efforts in the development of oleanolic acid and its analogs during the period from 2017 to 2020. Reports published during this period revealed that both OA and its analogs possess a remarkable potential for the development of effective anticancer agents along with several others, such as anti-inflammatory, anti-viral, antimicrobial, and anti-diabetic agents.

Coronaviruses are RNA-infective viruses that could be considered principal players in universal high-profile outbreaks, namely the Severe Acute Respiratory Syndrome (SARS, 2002-2003), the Middle East Respiratory Syndrome (MERS, 2012) and the continuing novel coronavirus disease (COVID-19, 2019) pandemic. RNA coronaviruses infections raise public health concerns with infections’ severity ranging from serious pandemics and highly contagious infections to common influenza episodes. With a wide consensus concerning the seminal role of early detection of the infectious agent on the clinical prognosis, recent technological endeavors have facilitated the rapid, sensitive and specific diagnosis of viral infections. Given that the burst of confirmed cases of the novel coronavirus disease 2019 (COVID-19) are climbing steeply, and we are amid this pandemic, this work will center at the respiratory RNA-viruses outbreaks, including the three coronaviruses-related pandemics, emphasizing on the approved diagnostic approaches, outlining therapeutic clinical trials as well as vaccine candidates. Based on the accumulated data and knowledge on the previous RNA-virus outbreaks, this review aspires to link the current intervention measures against SARS-CoV-2 infection with the previous interventions and to provide a roadmap for any possible future measures.

Lung Cancer (LC) is the leading cause of cancer deaths worldwide. Recent research has also shown LC as a genomic disease, causing somatic mutations in the patients. Tests related to mutational analysis and genome profiles have lately expanded significantly in the genetics/genomics field of LC. This review summarizes the current knowledge about different signalling pathways of LC based on the clinical impact of molecular targets. It describes the main molecular pathways and changes involved in the development, progression, and cellular breakdown of LC and molecular changes. This review focuses on approved and targeted experimental therapies such as immunotherapy and clinical trials that examine the different targeted approaches to treating LC. We aim to clarify the differences in the extent of various genetic mutations in DNA for LC patients. Targeted molecular therapies for LC can be continued with advanced racial differences in genetic changes, which have a significant impact on the choice of drug treatment and our understanding of the profile of drug susceptibility/ resistance. The most relevant genes described in this review are EGFR, KRAS, MET, BRAF, PIK3CA, STK11, ERBB3, PTEN, and RB1. Combined research efforts in this field are required to understand the genetic difference in LC outcomes in the future.

Background: Ziziphus oenoplia Mill. (Family- Rhamnaceae) an important shrub, often found throughout the hot regions of tropical Asia and northern Australia, is commonly well known as Jackal jujube in English. It is a folk herbal medicine used as an abdominal pain killer and antidiarrhoeal agent. Objective: The review aims to provide up-to-date information on the vernacular information, botanical characterization, distribution, ethnopharmacological uses, pharmacological activities, and chemical constituents of Z. oenoplia for possible exploitation of treatment for various diseases and to suggest future investigations. Methods: This review was performed by studying online resources relating to Z. oenoplia and diverse resources, including scientific journals, books, and worldwide accepted databases from which information was assembled to accumulate significant information and relevant data in one place. Results: Investigations on Z. oenoplia have been focused on its pharmacological activities, including its antimicrobial, antidiabetic, antihepatotoxic, antiulcer, antiplasmodial, anticancer, wound healing, anthelmintic, antioxidant, analgesic and antinociceptive, hypolipidemic activity, anti-inflammatory, immunomodulatory and antidiarrheal activities. Phytochemical studies resulted in the isolation of fatty acids, flavonoids, phenols, pentacyclic triterpenes, hydroxycarboxylic acids, aliphatic hydroxy ether, and cyclopeptide alkaloids. Conclusion: Most of the ethnopharmacological relevance of Z. oenoplia is justified, but more studies are needed. Further investigations are necessary to fully understand the mode of action of the active constituents and to exploit its preventive and therapeutic potentials.

Carbohydrazides and their Schiff bases are important classes of heterocycles that are not only employed in the area of organic chemistry but also have tremendous applications in physical and inorganic chemistry. A series of potentially bioactive compounds containing carbohydrazide functionality and their hydrazone derivatives have been synthesized and screened for antibacterial, anticancer, antifungal and anti-inflammatory, etc. This brief review discloses some synthetic routes to so many reported carbohydrazides, their Schiff bases, their biological activities, and their structure-activity relationship.