Design and Synthesis of Various Aryl Amide Derivatives of Imidazo[1,5-a] Pyridine-1,2,4-Thiadiazoles: In Vitro Cytotoxicity Evaluation and In Silico Molecular Docking Studies.

A new series of various aryl amide derivatives of imidazo[1,5-a]pyridine-1,2,4-thiadiazoles (15a-j) were designed, synthesized, and evaluated for their cytotoxic profiles against four human cancer cell lines such as breast cancer (MCF-7), lung cancer (A549), colon cancer (Colo-205), and ovarian cancer (A2780), via the MTT assay, with etoposide as the standard known chemotherapeutic agent. Five compounds, 15a, 15b, 15c, 15f, and 15j, exhibited more potent cytotoxic effects than did etoposide. Among them, compound 15a exhibited potent cytotoxic effects against the MCF-7, A549, Colo-205, and A2780 cell lines, with IC values of 0.

Recent advances and future perspectives in the therapeutics of prostate cancer.

Prostate cancer (PC) is one of the most common cancers in males and the fifth leading reason of death. Age, ethnicity, family history, and genetic defects are major factors that determine the aggressiveness and lethality of PC. The African population is at the highest risk of developing high-grade PC.

The role of NF-κB in breast cancer initiation, growth, metastasis, and resistance to chemotherapy.

Breast cancer (BC) is the second most fatal disease and is the prime cause of cancer allied female deaths. BC is caused by aberrant tumor suppressor genes and oncogenes regulated by transcription factors (TFs) like NF-κB. NF-κB is a pro-inflammatory TF that crucially alters the expressions of various genes associated with inflammation, cell progression, metastasis, and apoptosis and modulates a network of genes that underlie tumorigenesis.

Ultrasound assisted Cu-catalyzed Ullmann-Goldberg type coupling-cyclization in a single pot: Synthesis and evaluation of 11-pyrido[2,1-]quinazolin-11-ones against SARS-CoV-2 RdRp.

The evaluation of 11-pyrido[2,1-]quinazolin-11-one derivatives against SARS-CoV-2 RdRp was undertaken based on the reports on antiviral activities of this class of compounds in addition to the promising interactions of the antiviral drug penciclovir as well as quinazoline derivatives with SARS-CoV-2 RdRp . The target compounds were prepared an Ullmann-Goldberg type coupling followed by the subsequent cyclization (involving amidation) in a single pot. The methodology involved a CuI-catalyzed reaction of 2-iodobenzoate ester with 2-aminopyridine or quinolin-2-amine or thiazol-2-amine under ultrasound to give the expected products in acceptable (51-93%) yields.

assessment and sonochemical synthesis of 2-alkynyl 3-chloropyrazines as prospective ligands for SARS-CoV-2.

The recent global pandemic caused by COVID-19 has triggered an intense effort worldwide towards the development of an effective cure for this disease. In our effort we have explored the 2-alkynyl substituted 3-chloropyrazine framework as a potential template for the design of molecules for this purpose. Our strategy was supported by the studies of representative compounds to assess their binding affinities docking into the N-terminal RNA-binding domain (NTD) of N-protein of SARS-CoV-2.