Design, synthesis, and biological evaluation of novel pyrimidine derivatives as CDK2 inhibitors

Synthesis of Biginelli Compounds Using Cobalt Hydrogen Sulfate

“…1 The THPMs and their derivatives have shown a wide scope of important pharmacological and biological properties including antibacterial, antifungal, antiviral, antitubercular, anticancer and anti-malarial properties. [2][3][4][5] Due to the biological importance of THPMs, several new and improved procedures by applying microwave, 6 ultrasound 6 or UV irradiations 7 in the presence of various catalysts have been reported. Although many of these methods gave pure tetrahydropyrimidinones in good to excellent yields, but in most cases urea and ethyl acetoacetate were only used as reactants for the synthesis of 5-carboethoxy-2-oxo-1,2,3,4-tetrahydropyrimidines.…”

Synthesis and Biological Evaluation of Some New Naphthyl Derivatives as Anti-microbial Activity

“…The structure of compound 1 was confirmed from its infrared spectrum which revealed the presence of absorption bands due to υNH at 3348 cm -1 , υC-H at 2924cm -1 , υC=N at 1650 cm -1 , υC=C aromatic at 1624 cm -1 and υCH 3 at 1375 cm -1 . The 1 H-NMR (DMSO-d 6 ) spectrum of compound 1 showed signals at δ 2.31(3H, s, CH 3 ), δ7.2-8.13 (12H, m, Ar-H) and δ 10.71(1H, s, NH) ppm.…”

“…On the other hand the reaction of 1-acetyl naphthalene with thiosemicarbazide in pyridine gave the corresponding 1-methylnaphthyl thiosemicarbazide derivative 2. The structure of compound 2 was derived from its infrared spectrum which revealed the presence of υNH 2 at 3390 cm -1 , υNH at 3223 cm -1 ,υC=S at 2154 cm -1 , υC=N at 1643 cm -1 , υC=C at 1625 cm -1 and υCH 3 at 1373 cm -1 . The 1 H-NMR (DMSO-d 6 ) spectrum of compound 2 showed signals at δ2.10 (3H,s,CH 3 ), δ 6.88-7.64 (7H, m, Ar-H), δ 9.43 (2H, s, NH 2 ) and δ 11.1(1H, s, NH) ppm.…”

Novel 1,5-diphenyl-6-substituted 1H-pyrazolo[3,4-d]pyrimidin-4(5H)-ones induced apoptosis in RKO colon cancer cells

“…Encouraged by the above-mentioned findings and in continuation of our efforts linked with discovering and exploring novel lead structures as potent chemotherapeutic agents [23][24][25][26] , it was attempted to synthesize new pyrazolo [3,4-d]pyrimidin-4-ones comprising a variety of substituents at position 6 (E; Figure 1) to be evaluated for their anti-cancer activity. The substituents at position 6 include various pharmacophores and functionalities that are believed to be responsible for the biological significance of some relevant anti-cancer agents such as alkylamino 22,27 together with other pharmacophoric groups that would confer different electronic and lipophilic environment, which would influence the targeted anti-cancer activity. Since many guanidines were reported to possess cytotoxic and apoptosis inducing activities [28][29][30] , we deemed it interesting to explore the effect of introducing guanidino and aminoguanidino moieties at position 6.…”