Potentials of N-Acyl hydrazones Against Colorectal Cancer: A Mini Review.

Colorectal cancer (CRC) is a malignant gastrointestinal tract disorder with high occurrence and mortality index and showing an upsurge. Standard therapies for treating CRC are surgery and chemotherapy. Despite great effort in developing effective treatments, the progress is limited due to its relapse and recurrence.

Breaking barriers: enhancing solubility and dissolution of efonidipine using co-amorphous formulations.

The study aims to enhance the solubility and dissolution characteristics of efonidipine hydrochloride ethanolate (EFD), an antihypertensive drug, through the co-amorphous approach. Hypertension is a prevalent chronic condition characterized by consistently elevated blood pressure. Efonidipine, a BCS class II drug, has high permeability but low solubility, limiting its therapeutic effectiveness.

Thiazolotriazoles As Anti-infectives: Design, Synthesis, Biological Evaluation and Studies.

The rational design of novel thiazolo[2,3-][1,2,4]triazole derivatives was carried out based on previously identified antitubercular hit molecule H127 for discovering potent compounds showing antimicrobial activity. The designed compounds were screened for their binding efficacies against the antibacterial drug target enoyl-[acyl-carrier-protein] reductase, followed by prediction of drug-likeness and ADME properties. The designed analogues were chemically synthesized, characterized by spectroscopic techniques, followed by evaluation of antimicrobial activity against bacterial and fungal strains, as well as antitubercular activity against and strains.

Salazinic Acid and Norlobaridone from the Lichen : Antioxidant Activity, α-Glucosidase Inhibitory and Molecular Docking Studies.

The present study was intended for the identification of secondary metabolites in acetone extract of the lichen using UPLC-ESI-QToF-MS/MS and the detection of bioactive compounds. This study led to the identification of 22 metabolites based on their MS/MS spectra, accurate molecular masses, molecular formula from a comparison of the literature database (DNP), and fragmentation patterns. In addition, potent antioxidant and α-glucosidase inhibitory potentials of acetone extract of motivated us to isolate 10 metabolites, which were characterized as salazinic acid (), norlobaridone (), atranorin (), lecanoric acid (), lichesterinic acid (), protolichesterinic acid (), methyl hematommate (), iso-rhizonic acid (), atranol (), and methylatratate ( based on their spectral data.

Synthesis of aminomethyl linked (+)-usnic acid derivatives the Mannich reaction and evaluation of their biological activities.

(+)-Usnic acid (UA), a natural dibenzofuran derivative, abundantly produced by lichens and possess wide number of biomedical applications including antibacterial, anti-inflammatory, anti-oxidant and anticancer activities. In the present study, as series of usnic acid derivatives () were synthesised using Mannich reaction assessed for their antioxidant, α-glucosidase, and anticancer activities. The antioxidant activity showed that compound displayed potent antioxidant activity by scavenging the activities of DPPH and ABTS.

Synthetic and Medicinal Chemistry Approaches Toward WEE1 Kinase Inhibitors and Its Degraders.

WEE1 is a checkpoint kinase critical for mitotic events, especially in cell maturation and DNA repair. Most cancer cells' progression and survival are linked with elevated levels of WEE1 kinase. Thus, WEE1 kinase has become a new promising druggable target.

Development of 2-chloroquinoline based heterocyclic frameworks as dual inhibitors of SARS-CoV-2 M and PL.

Evolution of new variants of SARS-CoV-2 warrant the need for the continued efforts in identifying target-oriented new drugs. Dual targeting agents against M and PL not only overcome the incomplete efficacy but also the drug resistance, which is common problem. Since both these are cysteine proteases, we designed 2-chloroquinoline based molecules with additional imine moiety in the middle as possible nucleophilic warheads.

Scaffold identification and drug repurposing for finding potential Dengue envelope inhibitors through ligand-based pharmacophore model.

Most of the existing DENV entry inhibitors were discovered through structure-based, high-throughput screening techniques and optimization approaches by aiming β-OG pocket. However, the class of precise chemical scaffolds with superior antiviral activity targeting the early stages of virus infection that is considered to be beneficial in therapeutics and is still in process. In this study, ligand-based pharmacophore modeling using existing DENV entry inhibitors provided two best models, AADRR-2 and AAADR-2 (A- accepter, D- donor, R-ring) to screen public and DrugBank datasets.

Synthesis of novel thiazoles bearing lupeol derivatives as potent anticancer and anti-inflammatory agents.

Lupeol is one of the most important metabolite in the class of terpenoids and possess excellent anticancer, anti-inflammatory, anti-diabetic activities etc. In the present study, the different thiazoles and oxazoles bearing lupeol derivatives were prepared to enhance their biological activity. Initially, the cytotoxic activity results showed that the synthesized lupeol derivatives ( and ) showed significant activity against various cancer cells and the compounds and exhibited excellent activity against CAL27 cells.

Role of Dynamic Magnetic Resonance Imaging in Hirayama Disease, a Rare Motor Neuron Disease.

Introduction Hirayama disease (HD) is a benign self-limiting motor neuron disease, most commonly occurring in young males. The disease has an insidious onset that affects T1, C8, and C7 myotomes. HD is more common in Japan and Asian countries, and rare in the western population.

Synthesis and evaluation of novel almazole D analogs as anticancer agents.

Novel almazole D-amide conjugates, esters, and N-alkylated analogs were synthesized and investigated for their anticancer activity against seven cancer cell lines. Among the series, compounds 5g and 5m showed significant anticancer activities against multiple cell lines with moderate selectivity indices. Compound 5g had IC values of 5.

Design, synthesis and cytotoxic activity studies of alkyne linked analogues of Nimbolide.

A series of novel nimbolide derivatives bearing various substitutions on 28th position was designed and synthesized using Sonogashira (2a-2p) and Glaser coupling (3a-3e) reactions. The synthesized derivatives were assessed for in vitro cytotoxic activity against four different human cancer cell lines (A549 cells, MCF-7 cells, MDA-MB-231 cells, and HCT15 cells) and normal cell line (HEK cells) using MTT assay. Among the screened derivatives, the compound 3a showed potent activity against A549 cells with IC value of 0.

Synthesis and Anti-Cancer Activity of New Pyrazolinyl-Indole Derivatives: Pharmacophoric Interactions and Docking Studies for Identifying New EGFR Inhibitors.

Newly designed series of indole-containing pyrazole analogs, pyrazolinylindoles, were synthesized, and their structures were confirmed based on the spectral data of the H NMR, C NMR, and HR-MS analyses. Preliminary anti-cancer activity testings were carried out by the National Cancer Institute, United States of America (NCI, USA). Compounds HD02, HD05, and HD12 demonstrated remarkable cytotoxic activities against nine categories of cancer types based cell line panels which included leukemia, colon, breast, melanoma, lungs, renal, prostate, CNS, and ovarian cancer cell lines.

Continuous flow process for preparing budesonide.

Budesonide, a glucocorticosteroid, is used as anti-asthmatic drug that became generic in 2019. Existing preparation methods of budesonide require utilization of corrosive acids and involve expensive purification process. Thus, a new cost-effective continuous flow process for the synthesis of budesonide which belongs to the class of 16,17 acetals of pregnane core, is discussed in the present research findings.

Machine Learning in Drug Discovery: A Review.

This review provides the feasible literature on drug discovery through ML tools and techniques that are enforced in every phase of drug development to accelerate the research process and deduce the risk and expenditure in clinical trials. Machine learning techniques improve the decision-making in pharmaceutical data across various applications like QSAR analysis, hit discoveries, de novo drug architectures to retrieve accurate outcomes. Target validation, prognostic biomarkers, digital pathology are considered under problem statements in this review.

3-Aryl-substituted imidazo[1,2-a]pyridines as antituberculosis agents.

Novel inhibitors are needed to tackle tuberculosis. Herein, we report the 3-aryl-substituted imidazo[1,2-a]pyridines as potent antituberculosis agents. A small library of 3-aryl-substituted imidazo[1,2-a]pyridines was synthesized using direct arylation, followed by nitro reduction and finally Pd-catalyzed C-N coupling reactions.

A perspective on medicinal chemistry approaches towards adenomatous polyposis coli and Wnt signal based colorectal cancer inhibitors.

Colorectal cancer (CRC) is one of the major causes of carcinogenic mortality in numbers only after lung and breast cancers. The mutations in adenomatous polyposis coli (APC) gene leads to formation of colorectal polyps in the colonic region and which develop as a malignant tumour upon coalition with patient related risk factors. The protein-protein interaction (PPI) of APC with Asef (A Rac specific guanine nucleotide exchange factor) overwhelms the patient's conditions by rapidly spreading in the entire colorectal region.

Structure-based discovery of small molecule APC-Asef interaction inhibitors: In silico approaches and molecular dynamics simulations.

Colorectal cancer, which is considered one of the leading causes of mortality worldwide, develops through the formation of benign polyps on the inner colon or rectum wall. Truncations in adenomatous polyposis coli (APC) gene lead to the spread of the disease in the entire colon region when combined with the guanine nucleotide exchange factor (GEF) Asef. A series of peptidomimetic agents were previously discovered as protein-protein interaction inhibitors that can target the APC-Asef interface.

Cricket ball in the right heart: A case report of right atrial myxoma.

Introduction: Myxomas are the most common type of cardiac benign tumors and most of them are located in the left atrium, followed by the right atrium. The majority of Myxomas is located in the left atrium and has a variable clinical presentation. Myxomas affect patients within a wide age range (15-80 years), and the average age is approximately 50 years.

Rare case of aortic aneurysm with type A dissection (extending to right coronary artery) and severe AR in a nonhypertensive and non pregnant female.

Introduction: Typically a patient with acute aortic dissection presents with severe chest pain radiating to the back, tearing in nature. Rarely it can present as painless acute aortic dissection this is seen in iatrogenic cases or when associated with atherosclerosis, diabetes, or aortic aneurysm.

Case Presentation: We hereby present a case of a 32-year aged female who presented with dyspnoea & palpitations (NYHA III) from last 6 months, diagnosed to have Aortic Aneurysm with Type A dissection & Severe AR.