24451-15-8Relevant articles and documents
Structural insight into the reaction mechanism of Pd-catalyzed nitrile hydration: Trapping the [Pd(H2O)4]2+cation through a supramolecular complex
Fortea-Pérez, Francisco Ramón,Neve, Francesco,Armentano, Donatella,De Munno, Giovanni,Stiriba, Salah-Eddine,Julve, Miguel
, p. 267 - 273 (2016)
Four new bis(oxamato)palladate(II) complexes of formula (n-Bu4N)2[Pd(2,4,6-Me3pma)2]·2CH3CN (1), (n-Bu4N)2[Pd(2,4,6-Me3pma)2]·2CH3CONH2(2) and (n-Bu4N)4[Pd(H2O)4][Pd(4-Xpma)2]3·2CH3CONH2with X?=?Br (3) and Cl (4) (2,4,6-Me3pma?=?N-2,4,6-trimethylphenyloxamate, 4-Brpma?=?N-4-bromophenyloxamate, N-4-chlorophenyloxamate and n-Bu4N+?=?tetra-n-butylammonium) have been obtained and characterized by single crystal X-ray diffraction. All of them contain bis(oxamato)palladate(II) anions and bulky n-Bu4N+cations, but compounds 3 and 4 have also the out of the ordinary [Pd(H2O)4]2+inorganic cation. Acetonitrile and appealing acetamide are present as lattice molecules in compounds (1) and (2–4), respectively. While 1 was prepared in a neutral solution, species 2–4 were obtained in a basic medium. The acetamide molecules are the natural consequence of the acetonitrile hydration reaction during the oxamate-palladate(II) complexation. Interestingly, the use of a different oxamate ligand supports (through a molecular-recognition interaction) the structural grasping of the [Pd(H2O)4]2+species, which can be considered as a reaction intermediate for the nitrile hydration.
Design, synthesis and biological evaluation of 1-Aryl-5-(4-arylpiperazine-1-carbonyl)-1H-tetrazols as novel microtubule destabilizers
Wang, Chao,Li, Yuelin,Liu, Zi,Wang, Zeyu,Liu, Zihan,Man, Shuai,Zhang, Yujing,Bao, Kai,Wu, Yingliang,Guan, Qi,Zuo, Daiying,Zhang, Weige
, p. 549 - 560 (2021/02/05)
A series of 1-aryl-5-(4-arylpiperazine-1-carbonyl)-1H-tetrazols as microtubule destabilizers were designed, synthesised and evaluated for anticancer activity. Based on bioisosterism, we introduced the tetrazole moiety containing the hydrogen-bond acceptors as B-ring of XRP44X analogues. The key intermediates ethyl 1-aryl-1H-tetrazole-5-carboxylates 10 can be simply and efficiently prepared via a microwave-assisted continuous operation process. Among the compounds synthesised, compound 6–31 showed noteworthy potency against SGC-7901, A549 and HeLa cell lines. In mechanism studies, compound 6–31 inhibited tubulin polymerisation and disorganised microtubule in SGC-7901 cells by binding to tubulin. Moreover, compound 6–31 arrested SGC-7901cells in G2/M phase. This study provided a new perspective for development of antitumor agents that target tubulin.
NOVEL HETEROARYL COMPOUND, ENANTIOMER, DIASTEREOMER OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, AND ANTIVIRAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT
-
Paragraph 0823; 0824, (2020/02/14)
The present invention relates to a novel heteroaryl compound, an enantiomer, a diastereomer or a pharmaceutically acceptable salt thereof, and an antiviral composition comprising the same as an active ingredient. The novel compounds represented by formula (I) or formula (II) according to the present invention are remarkably superior in antiviral activity against an influenza virus, and furthermore, have low cytotoxicity and thus low adverse effects on a human body. Therefore, a pharmaceutical composition containing the same as an active ingredient can be effectively used for the prevention or treatment of diseases caused by an influenza virus infection.
