The current review concentrates on the latest breakthroughs of triazole-pyrimidines as target-based anticancer representatives, including works posted between 2007 and the current (2007-2022). The structure-activity interactions (SARs) and several paths will also be evaluated to reveal the development of more efficient and biotargeted anticancer candidates.In modern-day medication discovery and development, the prodrug strategy became a crucial technique for improving the pharmacokinetic profiles of drugs. A prodrug is a chemical compound, which gets metabolized into a pharmacologically active type (drug) within the body following its administration. In today’s work, we report ‘smProdrugs’ (http//cheminfolab.in/databases/prodrug/), which will be one of the primary unique databases on little molecule prodrugs. It stores the structures, physicochemical properties and experimental ADMET data manually curated from literary works. SmProdrugs lists 626 little molecule prodrugs and their particular energetic compounds aided by the previously discussed experimental data from 1808 study articles and 61 patents have already been saved. The details page of every record gives the frameworks and properties of the prodrug in addition to active medication side by side which makes it easy for the user to instantly compare them. The architectural improvements within the prodrug/active medications tend to be showcased in a different sort of colour for simple contrast. Experimental data happens to be curated through the installed PubMed and patent articles and had been catalogued in a tabular form with more than 25 fields under sub-sections i) title and structures associated with the prodrugs and their particular active compounds, ii) mode of activation associated with prodrug and enzyme/biocatalyst involved in the conversion, iii) indications/disease, iv) pharmacological target, v) experimental pharmacokinetic properties such solubility, consumption, volume of distribution, half-life, clearance etc. and vi) information about the purpose/gain from the prodrug techniques. Considering the ever growing utility regarding the prodrug strategy smProdrugs will undoubtedly be of great use to the systematic neighborhood working on logical design of tiny molecule prodrugs.COVID-19 is a complex disease with short-term and long-term breathing, inflammatory and neurological symptoms being set off by the disease with SARS-CoV-2. As much medications concentrating on single goals revealed only limited effectiveness against COVID-19, here, we aimed to explore a multi-target method. We synthesized a focused element library according to C2-substituted indolealkylamines (tryptamines and 5-hydroxytryptamines) with activity for three potential COVID-19-related proteins, specifically melatonin receptors, calmodulin and human angiotensin changing chemical 2 (hACE2). Two molecules through the library, 5e and h, exhibit affinities within the large nanomolar range for melatonin receptors, prevent the calmodulin-dependent calmodulin kinase II activity together with relationship of the SARS-CoV-2 Spike protein with hACE2 at micromolar levels. Both substances inhibit SARS-CoV-2 entry into host cells and 5h decreases SARS-CoV-2 replication and MPro enzyme activity in addition. In summary, we offer a proof-of-concept when it comes to effective design of multi-target substances in line with the tryptamine scaffold. Optimization of the initial hit compounds may potentially offer medication prospects to treat COVID-19 as well as other coronavirus diseases.The anion exchanger necessary protein SLC26A3 (down-regulated in adenoma, DRA) is expressed in the luminal membrane layer of intestinal epithelial cells in colon, where it facilitates the consumption of Cl- and oxalate. We formerly identified a 4,8-dimethylcoumarin class of SLC26A3 inhibitors that act from the SLC26A3 cytoplasmic surface, and demonstrated their particular effectiveness in mouse types of constipation and hyperoxaluria. Here, screening of 50,000 new compounds and 1740 substance analogs of active compounds through the major display produced five unique courses of SLC26A3-selective inhibitors (1,3-dioxoisoindoline-amides; N-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)acetamides; thiazolo-pyrimidin-5-ones; 3-carboxy-2-phenylbenzofurans and benzoxazin-4-ones) with IC50 down seriously to 100 nM. Kinetic washout and onset of action researches disclosed an extracellular site of action for the thiazolo-pyrimidin-5-one and 3-carboxy-2-phenylbenzofuran inhibitors. Molecular docking computations revealed putative binding sites for these inhibitors. In a loperamide type of irregularity in mice, orally administered 7-(2-chloro-phenoxymethyl)-3-phenyl-thiazolo [3,2-a]pyrimidin-5-one (3a) significantly increased stool body weight, pellet number and water content. SLC26A3 inhibitors with an extracellular web site of action offer the potential for creating non-absorbable, luminally acting inhibitors with reduced systemic visibility after dental administration. Our conclusions also declare that inhibitors of related SLC26 anion transporters with an extracellular site of activity might be identified for pharmacological modulation of selected epithelial ion transportation processes.Traditional chemotherapy and immunotherapy tend to be main disease-treatment techniques. Nonetheless, they face numerous challenges, including restricted healing benefits, off-target impacts, really serious negative effects, medication weight, long half-life time, poor dental bioavailability, and drugging undruggable proteins. Proteolytic targeted chimeras (PROTACs) were suggested to solve these issues. PROTACs tend to be heterogeneous functional abvos molecules linked by a chemical linker and contain a binding ligand when it comes to necessary protein interesting and a recruiting ligand for the E3 ligand. The binding of a PROTAC to a target necessary protein brings the E3 ligand enzyme into proximity, starting polyubiquitination regarding the target necessary protein, followed by protease-mediated degradation. Up to now, PROTACs against a large number of immunological goals happen effectively developed, many of which are medically validated drug targets, and many have entered clinical tests for immune-related diseases.