Synthesis and biological evaluation of 3-(piperidin-4-yl)isoxazolo[4,5-d]pyrimidine derivatives as novel PI3Kδ inhibitors

Crystal structure of 4-chloro-2-methyl-6-(4-(trifluoromethoxy)phenyl)pyrimidine, C12H8ClF3N2O

“…The pyrimidine nucleus, as well as other nitrogenous heterocyclic systems, have been considered in the design of various compounds with diverse biological properties, especially for the development of new anti-tumor agents [5][6][7][8].…”

Guidongnins I–J: Two New 6,7-seco-7,20-Olide-ent-kaurene Diterpenes with Unusual Structures from Isodon rubescens

“…Previously, the diterpenoids isolated from this species, such as oridonin, rosthorin, lushanrubescensin H, and rabdosin A, showed significant inhibitory activity against the growth of tumor cell lines [18]. Therefore, guidongnins I (1) and J (2) were evaluated for their cytotoxicities against various human cancer cell lines [A-549 (lung), HL-60 (leukemia), MCF-7 (breast), HepG2 (liver), and COLO-205 (colon)] using the CCK-8 method as previously reported [19][20][21]. The two compounds were inactive at a concentration of 100 µM, except for 2 on HepG2 cells.…”

“…The anti-proliferative activities of compounds 1-2 against human cancer cell lines were evaluated using the CCK-8 method, as previously described [18,19]. In the CCK-8 assay, the A549 cells were grown in Roswell Park Memorial Institute (RPMI) 1640 medium.…”

Novel Scaffolds Based on Bis-thiazole Connected to Quinoxaline or Thienothiophene through 2-Phenoxy-N-arylacetamide Groups as New Hybrid Molecules: Synthesis, Antibacterial Activity, and Molecular Docking Investigations

“…In this regard, thiazole derivatives have been shown to exhibit antiviral, antibacterial, antifungal, antidiabetic, antioxidant, anti-inflammatory, anticancer, and analgesic properties. − They are also found in 18 clinically approved drugs (FDA-approved), including antitumor drugs (epothilone and tiazofurin), anti-inflammatory drugs (meloxicam), antifungal drugs (isavuconazole), antiparasitic drugs (thiabendazole and nitazoxanide), antigout drugs (febuxostat), antithrombotic drugs (edoxaban), antiulcer drugs (nizatidine and famotidine), and antibacterial drugs (aztreonam, sulfathiazole, cefepime, and ceftriaxone) (Figure ). − Because of the simplicity of chemical achievement as well as structural optimization, thiazole-based scaffolds are the most attractive heterocycles in synthetic medicinal chemistry. ,, Furthermore, phenoxyacetamide and its derivatives are pharmacologically active molecules with anticancer, antiviral, antioxidant, anti-inflammatory, antiparasitic, antibacterial, and antihyperglycemic effects, as well as antituberculosis and MAO-A inhibitor activity. − AdipoRon VI (Figure ), a phenoxyacetamide medication, has received a lot of interest in this respect as a potential therapy for obesity, cardiovascular disease, diabetes, and nonalcoholic fatty liver disease. Moreover, quinoxaline derivatives have been the focus of substantial investigation since they have emerged as an important heterocyclic moiety with a varied spectrum of physicochemical and biological functions including antibacterial, antitubercular, antimalarial, antiviral, anti-inflammatory, antifungal, anticancer, antiproliferative, antitumor, and anticonvulsant properties. − They have a wide variety of biological actions.…”