- Synthesis and evaluation of antitumour activities of novel fused tri-And tetracyclic uracil derivatives
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Simple one-pot syntheses of indenopyrrolopyrimidines and indolopyrrolopyrimidines were achieved via the cyclocondensation of 6-Aminouracils and, respectively, ninhydrin and isatin in the presence of catalytic amounts of glacial acetic acid. Similarly, 5,6-diaminouracil derivatives were used as starting materials for the synthesis of indenopteridines and indolopteridines via their reaction with ninhydrin and isatin, respectively. The synthesised compounds were evaluated for antitumour activity against a human hepatocellular carcinoma cell line (HepG2), some showing antitumour activity comparable with 5-fluorouracil and imatinib.
- Elkalyoubi, Samar,Fayed, Eman
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p. 771 - 777
(2017/01/03)
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- Novel 2-thioxanthine and dipyrimidopyridine derivatives: Synthesis and antimicrobial activity
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Several fused imidazolopyrimidines were synthesized starting from 6-amino-1- methyl-2-thiouracil (1) followed by nitrosation, reduction and condensation with different aromatic aldehydes to give Schiff's base. The dehydrocyclization of Schiff's bases using iodine/DMF gave Compounds 5a-g. The methylation of 5a-g using a simple alkylating agent as dimethyl sulfate ((CH3)2SO4) gave either monoalkylated imidazolopyrimidine 6a-g at room temperature or dialkylated derivatives 7a-g on heating 6a-g with ((CH3)2SO4). On the other hand, treatment of 1 with different aromatic aldehydes in absolute ethanol in the presence of conc. hydrochloric acid at room temperature and/or reflux with acetic acid afforded bis-5,5′-diuracylmethylene 8a-e, which cyclized on heating with a mixture of acetic acid/HCl (1:1) to give 9a-e. Compounds 9a-e can be obtained directly by refluxing of Compound 1 with a mixture of acetic acid/HCl. The synthesized new compounds were screened for antimicrobial activity, and the MIC was measured.
- El-Kalyoubi, Samar,Agili, Fatmah,Youssif, Shaker
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p. 19263 - 19276
(2015/11/27)
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- Isolation, synthesis, and biological activity of aphrocallistin, an adenine-substituted bromotyramine metabolite from the hexactinellida sponge Aphrocallistes beatrix
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A new adenine-substituted bromotyrosine-derived metabolite designated as aphrocallistin (1) has been isolated from the deep-water Hexactinellida sponge Aphrocallistes beatrix. Its structure was elucidated on the basis of spectral data and confirmed throug
- Wright, Amy E.,Roth, Gregory P.,Hoffman, Jennifer K.,Divlianska, Daniela B.,Pechter, Diana,Sennett, Susan H.,Guzman, Esther A.,Linley, Patricia,McCarthy, Peter J.,Pitts, Tara P.,Pomponi, Shirley A.,Reed, John K.
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experimental part
p. 1178 - 1183
(2011/02/28)
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