432016-21-2Relevant articles and documents
Metal-Free Catalyzed Cyclization of N-Methoxybenzamides to Construct Quaternary Carbon-Containing Isoindolinones
Zhang, Lin-Bao,Wang, Zi-Chen,Sun, Sheng-Zheng,Ni, Shao-Fei,Wen, Li-Rong,Li, Ming
, p. 903 - 908 (2021)
Through the intramolecular cyclization of N-methoxybenzamides, a simple and efficient method for constructing valuable isoindolinones under metal-free conditions was developed. The reaction was featured by employing low-cost catalyst, simple operation, 100% atomic economy and excellent regioselectivity. Moreover, a detailed computational study on the reaction system has been performed to clarify the mechanism. This protocol tolerated a variety of functional groups and provided a metal-free protocol for the synthesis of chromane- or tetrahydroquinoline-fused isoindolinones in good yields.
Pyrazole compound, preparation method and application thereof, and pharmaceutical composition
-
Paragraph 0099-0105, (2020/07/08)
The invention relates to a substituted pyrazole compound, a preparation method and application thereof, and a pharmaceutical composition, wherein the pyrazole compound is represented by a formula (I),is an STAT3 signal channel inhibitor, and can be used for preventing and/or treating diseases related to STAT3 activity, such as tumors, autoimmune diseases, kidney diseases, cardiovascular diseases,inflammatory diseases, metabolic/endocrine dysfunction or neurological diseases.
Toluidinesulfonamide hypoxia-induced factor 1 inhibitors: Alleviating drug-drug interactions through use of pubchem data and comparative molecular field analysis guided synthesis
Wendt, Bernd,Mülbaier, Marcel,Wawro, Sabine,Schultes, Christoph,Alonso, Jorge,Janssen, Bernd,Lewis, Joe
experimental part, p. 3982 - 3986 (2011/08/05)
Inhibitors of hypoxia-inducible factor 1 (HIF-1) represent promising anticancer therapeutics. We have identified a series of potent toluidinesulfonamide HIF-1 inhibitors. However, the series was threatened by a potential liability to inhibit CYP2C9 which could cause dangerous drug-drug interactions when being coadministered with other drugs. We used structure-activity data from the PubChem database to develop a topomer CoMFAmodel that guided the design of novel sulfonamides with high selectivity for HIF-1 over CYP2C9 inhibition.
INHIBITORS OF CELL PROLIFERATION AND USES THEREOF
-
Page/Page column 30, (2009/10/21)
The present invention provides novel compounds that inhibit cell proliferation and uses of these compounds for treating, ameliorating or preventing diseases, conditions or disorders benefiting from the inhibition hyperproliferation.