Recent developments regarding the use of thieno[2,3-d]pyrimidin-4-one derivatives in medicinal chemistry, with a focus on their synthesis and anticancer properties

Medicinal Attributes of Thienopyrimidine Based Scaffold Targeting Tyrosine Kinases and Their Potential Anticancer Activities

“…It is generally understood that the antitumor properties of synthetic heterocyclic compounds are among the most powerful properties that can be made use of in medicinal chemistry. More specifically, their substantial cytotoxic effects against different types of human tumor cells, in addition to their roles as enzymes or receptors for various kinase inhibitors, make them critically important . Thiophene containing compounds are well known to exhibit various biological effects.…”

Synthesis, Characterization and Cytotoxicity of substituted[1]benzothieno[3,2-e][1,2,4]triazolo[4,3-a]pyrimidines

“…9,10 The presence of pyrimidine ring in the basic building scaffolds of DNA and RNA modules (thymine, cytosine and uracil) is probably the reason of their diverse biological activities. 11 In addition, the tricyclic system, cycloalkylthieno [2,3-d]pyrimidine, which is considered to be a bioisostere of quinazoline, has been used as a core for the mechanism-based design and synthesis of a variety of compounds for anticancer therapy.…”

Synthesis of novel heterocyclic fused pyrimidin-4-one derivatives from imino-1,2,3-dithiazoles

“…The thienopyrimidinone nucleus is known to be a pharmacologically relevant structure in medicinal chemistry and has generated interest from many research groups on account of its useful biological properties. For instance, the thieno [2,3-d]pyrimidinone substructure exhibits anticancer, [1][2][3][4][5] antimalarial 6 and antitubercular 7 activities. Some thieno [2,3-d]pyrimidin-(4)-ones act as selective phosphodiesterase inhibitors for the treatment of inflammatory diseases, 8,9 antagonists of the glutamate receptors 10 whereas others were identified as highly selective SIRT2 inhibitors.…”

“…11,12 Owing to their growing use in compounds of therapeutic importance, the synthesis of various thienopyrimidinone-based molecules has been actively pursued in the last past decade and studied in detail, leading to several new developments. 3,13,14 This skeleton is usually obtained by condensation and ring closure from various 2,3-substituted thiophenes such as Gewald's amide, 15 2-aminothiophene-3-carbonitrile, 16 3-carbethoxy-2-phenylthioureathiophene, 17 2-aminothiophene-3-carboxylic ester. 18 It is well known that reaction of 4,5-dichloro-1,2,3-dithiazolium chloride (2) (Appel's salt) with primary aromatic amines allows access to N-arylimino-1,2,3-dithiazoles, usually in high yield.…”