Cancer is one of the most prevailing disease conditions, which occurs due to uncontrolled cell division either due to natural mutation to the genes or due to changes induced by physical, chemical, or biological carcinogens. According to WHO, it is the second leading cause of death worldwide and has reported 10 million deaths in 2020. Hence, there arises the need for better chemotherapies and DNA intercalators are one such emerging therapy for cancer. DNA intercalating agents reversibly intercalate with the double‐helical structure of DNA by interacting with adjacent base pairs and disrupting the structure of DNA and thereby causing cell death. Here, we discuss the different classes of organo‐intercalators used in cancer therapy describing their anticancer and intercalation ability by different methods along with their structure–activity relationship and mechanism of action.

Indole moiety is a magnificent nucleus in the development of anticancer drugs. The pharmacological profile of indole is excellent in targeting a wide range of proteins, enzymes. An indole has a nitrogen atom that is capable of forming hydrogen bonds with the targets emphasizing its potential. Many studies have demonstrated the effectiveness of indole in the treatment of cancer by working through various pathways. Indole-based drugs got market approval to be used as chemotherapeutics, such as vincristine and vinblastine which encourage researchers to work on indole derivatives for cancer treatment with a better pharmacokinetic profile. This prompted us to review on indole derivatives as anticancer agents to bring out their potential derivatives under study. This study encompasses literature published between 2014 and 2021 on indole scaffold that exhibits in vitro and in vivo potential against cancer by searching PubMed, Google Scholar, and Science Direct databases. The search terms were "anticancer", "indole", "cell lines", "structure-activity relationship" and "cytotoxic activity."[a] A.

Insulin, on oral administration, is very troublesome because of its limited bioavailability. The evolution of oral insulin delivery formulations is greatly desired for non-invasive therapy by overcoming its low bioavailability, GIT enzymatic deactivation, poor lipophilicity and low stability. Different approaches have been proposed to boost oral insulin bioavailability in insulin-delivery systems and emerging effective therapies by using nanoparticle formulation, nanocapsid, modified chitosan particles, polydopamine microcapsules, and nanoliposomes. The present review includes patents and patent applications that were published between 2017 and January 2022.

Cirrhosis is a serious health condition, where along with scar tissue formation there is deposition of collagen in the liver, finally leading to liver failure. It is preceded by liver fibrosis, a dynamic pathological condition that can be decelerated during its early phases. Acute hepatitis is the cause of about 10% cases of liver damage and another 50% result from drug induced hepatic injury. In absence of appropriate clinical management of fibrosis, its progresses to cirrhosis and eventually results in liver failure or primary liver cancer both of which are irreversible conditions. Various in vivo animal models have been developed where hepatic injury is induced by diet, drugs, chemicals or surgical methods. These animal models are routinely employed for the assessment of drugs. But there is a need to discover new methods that will reduce animal sacrifice or be associated with animal recovery. Ex-vivo tissue culture techniques also aid in the evaluation of different stages of cirrhosis. Future research may result in the study of pathology of an individual patient through hepatic decellularisation and hepatic tissue bioengineering.

Background. Deficiency of insulin signaling in type 2 diabetes results from insulin resistance or defective insulin secretion and induce hyperglycemia. By reducing glycated hemoglobin, SGLT2 inhibitors improve hyperuricemia, blood lipids and weight loss without increasing the risk of hypoglycemia. By targeting this pathway, SGT2 inhibitors can become a prominent target in the management of type 2 diabetes. Objective. Interpretation of molecular docking and physicochemical properties of imidazo (2,1-b)-1,3,4 thiadiazole scaffold as SGLT2 inhibitors. Methods. The chemical structures of 108 molecules were drawn by using Chemdraw professional 15.0. Further, their energy minimization was also carried out by using Chem Bio Draw three-dimensional (3D) Ultra 12.0. Molecular docking was also carried out using a Molegro Virtual Docker to identify the best-fitting molecules and to identify the potential leads on the basis of dock score. The predicted parameters of drug-likeness according to Lipinski’s rule of five, such as molecular weight, log P, hydrogen bond acceptor, hydrogen bond donors, and number of rotatable bonds of the selected compounds, were predicted using pKCSM software. Results. 108 molecules were designed by employing different substitutions on imidazo-thiadiazole nucleus as SGLT2 inhibitors. Out of these 10 compounds were found to have better interactions with the active site of SGLT2 protein and the highest dock scores as compared to that of canagliflozin. Compounds 39a and 39b demonstrated good interactions and the highest dock score of -155.428 and -142.786 respectively. The insilicophysicochemical properties of the best compounds had also been determined. Additionally, these compounds suggested a good pharmacokinetic profile as per Lipinski's rule of five (orally active drugs). Conclusion. The imidazo (2,1-b)-1,3,4 thiadiazole scaffold was employed to design a novel SGLT2 inhibitor that exhibits maximum binding interactions with essential amino acids as well orally active.