13726-52-8Relevant articles and documents
FE NANOPARTICLES WITH PPM CONTENTS OF PD, CU AND/OR NI, REACTIONS IN WATER CATALYZED BY THEM
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Paragraph 0084; 0102, (2017/07/14)
The present application discloses a nanoparticle composition prepared from a mixture comprising: a) a transition metal salt; b) an iron salt; and c) a reducing agent; and methods for the use of such compositions, including the reduction of an organic compound comprising a nitro group to form an organic compound comprising an amine group, the Cu-catalyzed cyclization of an azide and an alkyne (click chemistry) and cross coupling reactions, notably Suzuki-Miyaura reactions. The transition metal salts are in particular Pd, Cu and Ni salts, the content of these metals being typically in the ppm range based on the major constituent Fe in the final products.
Novel 8-deaza-5,6,7,8-tetrahydroaminopterin derivatives as dihydrofolate inhibitor: Design, synthesis and antifolate activity
Zhang, Zhili,Wu, Jun,Ran, Fuxiang,Guo, Ying,Tian, Ran,Zhou, Shouxin,Wang, Xiaowei,Liu, Zhenming,Zhang, Liangren,Cui, Jingrong,Liu, Junyi
experimental part, p. 764 - 771 (2009/09/27)
We report, for the first time, the synthesis and biological activities of 8-deaza-5,6,7,8-tetrahydroaminopterin 9, and the 5-substituted and 5,10-disubstituted analogues 11, 13, 15, and 17. The analogues were obtained from key compound diethyl 8-deaza-5,6,7,8-tetrahydroaminopterin 8 following the catalytic reduction of the pyridine ring of diethyl 8-deaza aminopterin 5. The five novel 8-deaza-5,6,7,8-tetrahydroaminopterin derivatives were assayed in vitro for their cytotoxicity on BGC-823, HL-60, Bel-7402 and Hela tumor cell lines, and inhibition on recombinant human dihydrofolate reductase (DHFR), among which the most potent molecule (compound 9) was about 4- to 10-fold poorer than MTX on the four kinds of tumor cell lines, and its effect on DHFR was about 17-fold poorer than MTX. The docking studies were followed to explain the biological testing results.
A Potent Multisubstrate Analogue Inhibitor of Human Thymidylate Synthetase
Srinivasan, Ananthachari,Amarnath, Venkataraman,Broom, Arthur D.,Zou, F. C.,Cheng, Yung-Chi
, p. 1710 - 1717 (2007/10/02)
The synthesis of an 8-deazafolate analogue of the intermediate in the methylation of 2'-deoxyuridylate is described.Alkylation of diethyl 5,6,7,8-tetrahydro-8-deazafolate with 3'-O-acetyl-5-(bromomethyl)-2'-deoxyuridine 5'-, followed by removal of the trichloroethyl groups with a Zn/Cu couple and mild saponification, gave the target inhibitor N-pyridopyrimidin-6-yl>methyl>amino>benzoyl>-L-glutamic acid 5'-monophosphate.The free nucleoside and the 5'-(methyl phosphate) diester were similary prepared.Each of these reactions yielded a pair of diastereoisomers about C-6 of the reduced deazafolate in approximately a 1:1 ratio.These diastereomeric mixtures were evaluated as inhibitors of thymidylate synthetase derived from human tumor (HeLa) cells.The 5'-monophosphate was a potent inhibitor, competitive with respect to both 2'-deoxyuridylate (Ki = 0.06 μM) and tetrahydrofolate (Ki = 0.25 μM).In contrast, the nucleoside and the nucleotide methyl ester were poorer inhibitors by more than 3 orders of magnitude, attesting to the importance of the anionic function at the nucleoside 5'-position in the affinity of an inhibitor for the enzyme active site.
