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Anticancer activities of some newly synthesized pyrazole and pyrimidine derivatives
Ashraf M. Mohamed,Weal A. El-Sayed,Musaed A. Alsharari,Husam R. M. Al-Qalawi,Mousa O. Germoush 대한약학회 2013 Archives of Pharmacal Research Vol.36 No.9
A series of pyrazolopyridine and pyridopyrimidinederivatives 2–6 were newly synthesized using3,5-bisarylmethylene-1-methylpiperidone as the startingmaterial. The anticancer activities of the synthesizedcompounds were evaluated using 59 different human tumorcell lines, representing cancers of CNS, ovary, renal,breast, colon, lung, leukemia, and melanoma, prostate aswell as kidney. Some of the tested compounds, especiallythose with a fluorine substituent at the para-position in thephenyl ring and those with a pyridopyrimidine-2-thionewith a free –NH or –SH, exhibited greater in vitro antitumoractivities at low concentrations (log 10 [GI50] =-4.6) against the human tumor cell lines. Additionally,some of the compounds had moderate inhibitory effects onthe growth of the cancer cell lines. The detailed synthesis,spectroscopic data and antitumor properties of the synthesizedcompounds are reported.
Weal A. El-Sayed,Randa E. Abdel Megeid,Hebat-Allah S. Abbas 대한약학회 2011 Archives of Pharmacal Research Vol.34 No.7
New 1-[(tetrazol-5-yl)methyl]indole derivatives, their acyclic nucleoside analogs and the corresponding glycoside derivatives were synthesized. Furthermore, the [(1,2,4-triazol-3-yl)methyl]-2H-tetrazole derivative as well as the corresponding thioglucoside were prepared. The synthesized compounds were tested for their antimicrobial activity against Aspergillus Niger, Penicillium sp, Candida albican, Bacillus subtilis, Streptococcus lacti, Escherichia coli, Pseudomonas sp., and streptomyces sp. Compounds 3, 5 and 19b exhibited potent antibacterial activity and compounds 4, 5 and 10 exhibited high activities against the tested fungi compared with fusidic acid.