QUINAZOLINE DERIVATIVES AND QUINAZOLINE COMPLEX PROTEIN KINASE INHIBITOR FOR INHIBITING MULTIPLICAITON OF TUMOR CELLS AND PREPARATION METHOD THEREOF
申请人:Wang Fuyi
公开号:US20130225811A1
公开(公告)日:2013-08-29
Quinazoline derivatives represented by general formula (1) and quinazoline complexes as protein kinase inhibitors, and their preparation methods are provided. Wherein, in general formula (1), at least one of R and R′ is a group containing an atom capable of coordinating with noble metals, m and n are either the same or different and are integers from 0 to 5. Said quinazoline complex as protein kinase inhibitor is formed by coordination compound containing noble metal and said quinazoline derivative ligand capable of coordinating with noble metal in the coordination compound. Used as tyrosine protein kinase inhibitors, Quinazoline derivatives and quinazoline complexes as protein kinase inhibitors provided by the present invention have exhibited good inhibitory effect on proliferation of various tumor cells including human breast cancer cells line (drug-resistant) MCF-7/A, human breast cancer cell line (sensitive) MCF-7/S, prostate cancer cell PC-3, keratinocytes Colo-16, human non-small cell lung cancer cell line A549, etc.
本发明公开了一种大黄酸特定基团修饰的有机化合物及其金属配合物、及其制备方法和应用,与大黄酸分子相比,具有更好的抗肿瘤、抗菌活性,上述金属配合物还能诱导核酸构型转变。其中芳基金属二聚体、上述金属配合物均具有良好的抑制肥胖基因FTO(Fat Mass and Obesity Associated)活性,是很好的FTO抑制剂。本发明还公开了上述有机化合物及其金属配合物的合成方法,该方法工艺流程简单、易于操作,且产率高。本发明最后公开了上述含有大黄酸基团的有机化合物及其金属配合物、芳基金属二聚体在用于制备FTO抑制剂药物、FTO抑制剂药物组分、减肥药物、减肥药物组分、抗癌药物、抗癌药物组分、抗菌药物及抗菌药物组分方面的应用。
Charged Macromolecular Rhenium Bipyridine Catalysts with Tunable CO
<sub>2</sub>
Reduction Potentials
作者:Swagat Sahu、Po Ling Cheung、Charles W. Machan、Steven A. Chabolla、Clifford P. Kubiak、Nathan C. Gianneschi
DOI:10.1002/chem.201701901
日期:2017.6.27
acetonitrile under an inert atmosphere and with saturated CO2 indicate that the quaternaryammoniumpolymers exhibit a significantly lower potential for CO2 reduction to CO (ca. 300 mV), while neutral polymers behave consistently with what has been reported for the free, molecular catalyst. In contrast, the trifluoroborate polymers displayed a negative shift in potential and catalytic activity was not observed
[EN] CHEMICAL LIBRARIES USEFUL FOR DRUG DISCOVERY PROCESSES<br/>[FR] BIBLIOTHEQUES CHIMIQUES UTILES AUX PROCEDES DE DECOUVERTES DE MEDICAMENTS
申请人:7TM PHARMA AS
公开号:WO2003003008A1
公开(公告)日:2003-01-09
Use of chemical compounds or selections of chemical compounds (libraries) of the general formula (I): for in vivo methods for testing or validating the physiological importance and/or the therapeutic or pharmacological potential of biological target molecules, notably proteins such as, e.g., receptors and especially 7TM receptors in test animals expressing the biological target molecule with, notably, a silent, engineered metal-ion site. Use of specific metal-ion binding sites of a generic nature in specific biological target molecules such as, e.g. transmembrane proteins wherein the metal-ion binding site is capable of forming a complex with a metal ion is also described. Chemical compounds or libraries suitable for use in methods for improving the in vivo pharmacokinetic behaviour of metal-ion chelates (e.g. the absorption pattern, the plasma half-life, the distribution, the metabolism and/or the elimination of the metal-ion chelates). In order to improve the efficacy of the metal-ion chelates impact on the biological target molecule after administration of the metal-ion chelate in vivo to a test animal it is advantageous e.g. to increase the time period during which the metal-ion chelate is in the circulatory system and/or localised at the target. Metal-ion chelating compounds, which are designed to be suitable for use in a target validation process according to the invention and to libraries of at least two or more of such metal-ion chelating compounds are disclosed.