3749-47-1Relevant academic research and scientific papers
Synthesis and characterization of novel pyrimidine-4,5-diamine as anticancer agent
Maddur, Nagaraj,Rao, Cherukumalli Purna Koteswara,Rao, Maturi Someswara,Rao, Tadiboina Bhaskara
, p. 4334 - 4341 (2020/08/06)
Unlike latent cells, cancer cells supply deoxyribonucleoside triphosphates to cells continuously and thereby, prop up the uncontrolled cancer growth. Pyrimidine has been concerned in the separation of leukemic cells, known as adenine bioisosteres, as well as its biological activities, especially its anticancer properties. In this context, a novel series of N5-(3-substituted benzylidene)-N4-phenyl pyrimidine-4,5-diamine [5A-5F] / N5-(2-substituted benzylidene)-N2,N2-dimethyl-N4-phenyl pyrimidine-2,4,5-triamine [5a-5f] were synthesized by using the starting ingredient formimidamide/4(dimethylamino) benzimidamide and sodium ethoxide. The synthesized compounds were characterized by IR,1H NMR, and Mass spectral analyses and screened for their biological studies. In the present study, pyrimidine derivatives and their insilico modeling were done by using c-Src kinase and p38 MAP kinase complex followed by the evaluation of their anticancer activity. The screening of synthesized scaffolds possessed significant activity against HeLa cell lines and showed similar activity compared to standard Cisplatin. Among all the synthesized compounds, N5-(4-hydroxybenzylidene)-N4-phenyl pyrimidine-4,5-diamine 5A, N5benzylidene-N4-phenylpyrimidine-4,5-diamine 5C, N5-benzylidene-N2, N2-dimethyl-N4-phenyl pyrimidine-2,4,5-triamine 5c, and N5-(4-methoxy benzylidene)-N4-phenyl pyrimidine-4,5-diamine 5E showed the highest significant anticancer activity.
Synthesis and biological evaluation of pyrimidine derivatives as novel human Pin1 inhibitors
Cui, Guonan,Jin, Jing,Chen, Hualong,Cao, Ran,Chen, Xiaoguang,Xu, Bailing
, p. 2186 - 2197 (2018/03/28)
Pin1 (Protein interacting with NIMA1) is a cis–trans isomerase and promotes the amide bond rotation of phosphoSer/Thr-Pro motifs in its substrates. Inhibition of Pin1 might be a novel strategy for developing anticancer agents. Herein, a series of pyrimidi
Preparation method of nitroolefin derivatives
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Paragraph 0022, (2016/10/10)
The invention discloses a preparation method of nitroolefin derivatives.The method includes the following step of adding a vinyl compound, sodium nitrite, manganese dioxide and 2,2,6,6-tetramethylpiperidinyloxy to solvent to react at a temperature of 60-100 DEG C to obtain the nitroolefin derivatives.The vinyl compound serves as the reaction initiator, raw materials are easy to obtain and plentiful in species, the prepared target products nitroolefin derivatives can be directly used and can also be further used for being derived into other products; the industrial product sodium nitrite used serves as the nitration agent and is low in price and convenient and safe to use; the method is free of metal catalysts, mild in reaction condition, high in target product yield, small in pollution, low in production cost, simple in reaction operation and postprocessing process and suitable for industrial production.
Cephalosporin derivatives
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, (2008/06/13)
Penicillins and cephalosporins of the formula STR1 wherein A is phenyl, 4-hydroxyphenyl, cyclohexyl, cyclohene-1-yl, cyclohexa-1,4-diene-1-yl, 2-thienyl, 3-thienyl, 2-furyl, 3-furyl or 3,4-disubstituted phenyl, where the substituents, which may be identical to or different from each other, are each chlorine, hydroxyl or methoxy; R1 is an unsubstituted or substituted 5- or 6-membered heterocycle comprising carbon atoms and 1 to 4, preferably 1 to 2, identical or different heteroatoms such as oxygen, sulfur or nitrogen; n is 0 or 1; X is STR2 D is hydrogen, hydroxyl, acetoxy, aminocarbonyloxy, pyridinium, aminocarbonyl-pyridinium or S-Het, where Het is 1-methyl-tetrazol-5-yl, tetrazol-5-yl, 3-methyl-1,2,4-thiadiazol-5-yl, 1,2,4-triadiazol-5-yl, 1,3,4-thiadiazol-5-yl, 2-methyl-1,3,4-thiadiazol-5-yl, 2-methylamino-1,3,4-thiadiazol-5-yl, 2-dimethylamino-1,3,4-thiadiazol-5-yl, 2-formylamino-1,2,4-thiadiazol-5-yl, 2-acetylamino-1,3,4-thiadiazol-5-yl, 2-methyl-1,3,4-oxadiazol-5-yl, 1,2,3-triazol-4-yl or 1,2,4-triazol-3-yl; and E is hydrogen or a protective group which is easily removable in nitro or in vivo, especially an ester-forming group which can be removed under mild conditions by hydrogenation or hydrolysis or other treatments, or an ester-forming group which can easily be split off in the living organism; and, when E is hydrogen, their non-toxic, pharmacologically acceptable salts thereof, such as their alkali metal or alkaline earth metal salts, especially the sodium, potassium, magnesium or calcium salts; their ammonium salts; or their organic amine salts, especially the triethylamine or dicyclohexylamine salts. The compounds are useful as antibiotics.
