2293-75-6Relevant academic research and scientific papers
Synthesis, structure determination, and biological evaluation of phenylsulfonyl hydrazide derivatives as potential anti-inflammatory agents
Park, Eun Beul,Kim, Kwang Jong,Jeong, Hui Rak,Lee, Jae Kyun,Kim, Hyoung Ja,Lee, Hwi Ho,Lim, Ji Woong,Shin, Ji-Sun,Koeberle, Andreas,Werz, Oliver,Lee, Kyung-Tae,Lee, Jae Yeol
, p. 5193 - 5197 (2016/10/30)
In our previous research, a novel series of phenylsulfonyl hydrazide derivatives were found to reduce LPS-induced PGE2levels in RAW 264.7 macrophage cells via an inhibition of mPGES-1 enzyme. Recently, it was found that a regioisomeric mixture of phenylsulfonyl hydrazide was formed depending on the reaction conditions, which favor either of two regioisomers. One regioisomer corresponds to a kinetic product (7a–7c) and the other regioisomer corresponds to a thermodynamic product (8a–8c). Among them, the structure of kinetic product 7b was confirmed by measuring single X-ray crystallography. In vitro PGE2assay studies showed that the kinetic product (7a and 7b; IC50= 0.69 and 0.55 μM against PGE2) is generally more potent than the thermodynamic product (8a and 8b; IC50= >10 and 0.79 μM against PGE2). A molecular docking study also exhibited that the kinetic product (7a) has a higher MolDock Score (?147.4) than that of 8a (?142.4), which is consistent with the PGE2assay results. A new potent phenylsulfonyl hydrazide (7d; IC50= 0.06 μM against PGE2) without affecting COX-1 and COX-2 enzyme activities was identified based on these overall results.
NOVEL VINBLASTINE DERIVATIVES, THEIR PREPARATION, USE AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAID DERIVATIVES
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Page/Page column 45, (2009/12/05)
The invention provides vinblastine derivatives represented by the following formula 1 or their physiologically acceptable salts, their preparation, use and pharmaceutical compositions comprising the said derivatives. The said vinblastine derivatives show inhibiting activities against tumor cell lines and can be used as medicaments for treating malignant tumors.
Substituted acid derivatives useful as antidiabetic and antiobesity agents and method
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, (2008/06/13)
Compounds are provided which have the structure wherein Q is C or N, A is 0 or S, Z is O or a bond, X is CH or N and R1, R2, R2a, R2b, R2c, R3, Y, x, m, and n are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.
