Synthesis of novel pyrimidine and fused pyrimidine derivatives

Synthesis, antiproliferative activity, and molecular docking of some N‐heterocycles bearing a pyrazole scaffold against liver and breast tumors

“…[ 23,24 ] Recently, it was reported that 2‐cyano‐3‐arylacryloyl chlorides were utilized as building blocks for several heterocyclic skeletons like benzimidazoles, benzoxazoles, benzothiazoles, benzothiazepines, benzoxazinones, pyrimidinethiones, oxadiazoles, and pyrazoles with significant pharmaceutical potency. [ 25–29 ] Based on these facts, we aimed, in this work, to construct new pyrazole‐based heterocycles, for example, oxadiazepine, pyridopyrimidine, thiadiazolopyrimidine, and benzoxazinone derivatives, starting from acryloyl chloride derivative, and evaluate their antiproliferative efficacy against liver and breast cancer cells, as well as, the molecular docking study, using MOE (molecular modeling environment), to infer the binding free energies of the studied compounds toward the human cyclin‐dependent kinase 2.…”

Synthesis of Pyrazolo‐[4́,3́:5,6]pyrido[2,3‐d]pyrimidine‐diones Catalyzed by a Nano‐sized Surface‐Grafted Neodymium Complex of the Tungstosilicate via Multicomponent Reaction

“…Cancer is as a result of the uncontrolled growth of cells, tissue damage, invasion and metastases. The advances in drug discovery related to the cancer therapy is actually associated with the severe side effects, resistance to the conventional medicines, as well as an inadequate chemical space, leading to high demand for design and discovery of new chemotherapeutic medicines . So far, many efforts have been made for the discovery of new scaffolds, especially heterocyclic systems through both industrial and academic projects.…”

Synthesis and antimicrobial evaluation of some new quinazolin-4(3H)-one derivatives

“…In continuation of our interest in synthesis and studying the reaction behavior of benzoxazinones and quinazolinones [16][17][18][19][20] we reported herein the behaviour of the benzoxazinone derivative, 3, with some active methylene compounds as carbone nucleophile, so the benzoxazinone derivative, 3, was reacted with ethyl cyanoacetate and/or malononitrile in pyridine to give 2-(2-(anthracen-9-yl)-1-benzamidovinyl)-4-oxo-3,4-dihydro-quinoline-3-carboxylic acid, 6, via ring opening and ring closure of the benoxazinone derivative, 3, followed by hydrolysis of the cyano or the ethylester group to the carboxylic group. The structure of compound 6 was confirmed from the 1 H NMR spectrum showing the δ value at 12.48 ppm for singlet, one proton, corresponding to the carboxylic hydrogen and disappeared by D2O, hydrazinolysis of compound 3 in boiling ethanol afforded the triazinoquinqzolinone derivative, 7, according to the following mechanism (Scheme 3).…”