88636-52-6Relevant articles and documents
Exploring Heteroaryl-pyrazole Carboxylic Acids as Human Carbonic Anhydrase XII Inhibitors
Cadoni, Roberta,Pala, Nicolino,Lomelino, Carrie,Mahon, Brian P.,McKenna, Robert,Dallocchio, Roberto,Dessì, Alessandro,Carcelli, Mauro,Rogolino, Dominga,Sanna, Vanna,Rassu, Mauro,Iaccarino, Ciro,Vullo, Daniela,Supuran, Claudiu T.,Sechi, Mario
, p. 941 - 946 (2017)
We report the synthesis, biological evaluation, and structural study of a series of substituted heteroaryl-pyrazole carboxylic acid derivatives. These compounds have been developed as inhibitors of specific isoforms of carbonic anhydrase (CA), with potential as prototypes of a new class of chemotherapeutics. Both X-ray crystallography and computational modeling provide insights into the CA inhibition mechanism. Results indicate that this chemotype produces an indirect interference with the zinc ion, thus behaving differently from other related nonclassical inhibitors. Among the tested compounds, 2c with Ki = 0.21 μM toward hCA XII demonstrated significant antiproliferative activity against hypoxic tumor cell lines. Taken together, the results thus provide the basis of structural determinants for the development of novel anticancer agents.
Exploiting single-molecule magnets of β-diketone dysprosium complexes with C3v symmetry: Suppression of quantum tunneling of magnetization
Dong, Yanping,Yan, Pengfei,Zou, Xiaoyan,Liu, Tianqi,Li, Guangming
, p. 4407 - 4415 (2015)
A series of four β-diketone mononuclear dysprosium complexes, namely, Dy(EIFD)3(H2O)·CH2Cl2 (1), Dy(EIFD)3(DMF)·CH2Cl2 (2), Dy(EIFD)3(DMSO) (3), and Dy(EIFD)3/su
Synthesis and bioactivity assessment of novel spiro pyrazole-oxindole congeners exhibiting potent and selective in vitro anticancer effects
Abdelhamid, Sayeda A.,Abo-Salem, Heba M.,Aboul-Soud, Mourad A. M.,Al-Sheikh, Yazeed A.,Ebied, Manal S.,El-Sawy, Eslam R.,Elawady, Mohamed E.,Nassrallah, Amr,Soliman, Ahmed A. F.
, (2020/03/17)
The present work aims to design and synthesize novel series of spiro pyrazole-3,3'-oxindoles analogues and investigate their bioactivity as antioxidant and antimicrobial agents, as well as antiproliferative potency against selected human cancerous cell li
Rhodium(III)-catalyzed C4-amidation of indole-oximes with dioxazolones: Via C-H activation
Deng, Ke-Zuan,Fu, Xiao-Pan,Ji, Ya-Fei,Tang, Shi-Biao,Wu, Gao-Rong,Xia, Cheng-Cai,Yang, Jin-Yue,Zhang, Li-Li
supporting information, p. 7922 - 7931 (2020/11/02)
A novel method for the Rh(III)-catalyzed oxime-directed C-H amidation of indoles with dioxazolones has been developed. This strategy provides an exclusive site selectivity and the directing group can be easily removed. This transformation features a wide substrate scope, good functional group tolerance and excellent yields, and may serve as a significant tool to construct structurally diverse indole derivatives for the screening of potential pharmaceuticals in the future. This journal is