Targeting the α-folate receptor with cyclopenta[g]quinazoline-based inhibitors of thymidylate synthase

Green synthesis of 2-aryl-4-phenyl-quınazolıne derıvatives promoted by lactıc acıd

“…Prajapati and co-workers [9] have identified one of the intermediates, D (in Scheme 2), as the major product, which is formed from C upon cyclization. According to their proposed mechanism [9,10], C can be formed in two ways, in which the preferred first step was assumed to be the attack of NH 4 OAc on the keto group of the benzophenone moiety. …”

“…Specifically, quinazolines and their derivatives represent a medicinally and pharmaceutically important class of heterocyclic motifs that are found as the core structural skeletons in a variety of drug molecules such as prazosin [2] and lapatinib [3] (Figure 1). They possess a wide range of biological and pharmacological activities, including anticancer [4], antiviral [5], antitubercular [6] and antimalarial properties [7]. Zhang et al [8] have reported quinazoline synthesis with 2-aminobenzophenones and benzylic amines via SP 3 C-H activation, where I 2 served as a catalyst in the presence of an added oxidant at a relatively high temperature (90 °C) and relatively longer reaction time (12 h).…”

Time course gene expression in the one-carbon metabolism network using HepG2 cell line grown in folate-deficient medium

“…Folate deficiency is also associated with apoptosis [1] and cancer such as uterin cervix [2,3], lung and breast [4][5][6], and the colorectal one [7][8][9][10]. In addition, enzymes in the FOCM pathways such as dihydrofolate reductase (DHFR) and thymidilate synthase (TS) are targets of anti-cancer drugs [11][12][13]. Moreover, DNA-(5-methylcytosine)-methyltransferase (DNMT) and folate receptor (FR) are candidates as targets for chemotherapy [14,15].…”

Synthesis of a Novel Series of Thieno[3,2-d]pyrimidin-4-(3H)-ones

“…Chloroformamide hydrochloride was prepared in one step from cyanamide and anhydrous hydrogen chloride in excellent yield (Scheme 2). 5 The amino thiophenes esters (1a-g) were synthesized from b-chloropropenonitrile obtained from b-chloropropenal as described previously (Scheme 3). 6 Ethyl 3-aminothiophene-2-carboxylate (1h) was prepared from a-chloroacrylonitrile in excellent yield (90%; Scheme 4).…”