6373-23-5Relevant academic research and scientific papers
Synthesis of quinone imine and sulphur-containing compounds with antitumor and trypanocidal activities: Redox and biological implications
Almeida, Renata G.,Barbosa, Juliana M. C.,De Carvalho, Guilherme G. C.,De Castro, Solange L.,De Simone, Carlos A.,Goulart, Marilia O. F.,Kharma, Ammar,Paier, Carlos R. K.,Pessoa, Claudia,Pinheiro, Daniel P.,Da Silva Júnior, Eufranio N.,Rosa, Luísa G.,Valen?a, Wagner O.
, p. 1145 - 1160 (2020/11/03)
Ortho-Quinones represent a special class of redox active compounds associated with a spectrum of pronounced biological activities, including selective cytotoxicity and antimicrobial actions. The modification of the quinone ring by simple nitrogen and sulphur substitutions leads to several new classes of compounds with their own, distinct redox behaviour and equally distinct activities against cancer cell lines and Trypanosoma cruzi. Some of the compounds investigated show activity against T. cruzi at concentrations of 24.3 and 65.6 μM with a selectivity index of around 1. These results demonstrate that simple chemical modifications on the ortho-quinone ring system, in particular, by heteroatoms such as nitrogen and sulphur, transform these simple redox molecules into powerful cytotoxic agents with considerable "potential", not only in synthesis and electrochemistry, but also, in a broader sense, in health sciences. This journal is
Discovery of Small-Molecule Inhibitors of the HSP90-Calcineurin-NFAT Pathway against Glioblastoma
Liu, Zhenzhen,Li, Hongli,He, Lian,Xiang, Yu,Tian, Chengsen,Li, Can,Tan, Peng,Jing, Ji,Tian, Yanpin,Du, Lupei,Huang, Yun,Han, Leng,Li, Minyong,Zhou, Yubin
, p. 352 - 7,365 (2019/03/19)
Glioblastoma (GBM) is among the most common and malignant types of primary brain tumors in adults, with a dismal prognosis. Although alkylating agents such as temozolomide are widely applied as the first-line treatment for GBM, they often cause chemoresis
Discovery of naphtho[1,2-d]oxazole derivatives as potential anti-HCV agents through inducing heme oxygenase-1 expression
Tseng, Chih-Hua,Lin, Chun-Kuang,Chen, Yeh-Long,Tseng, Chin-Kai,Lee, Jar-Yu,Lee, Jin-Ching
, p. 970 - 982 (2017/12/15)
A number of naphtho[1,2-d]oxazole derivatives were synthesized and evaluated for their anti-HCV virus activity. Among them, compound 18 was the most active, exhibited approximately 21-folds more active anti-HCV activity (IC50 of 0.63 μM) than t
Selective Inhibitors of Human Liver Carboxylesterase Based on a β-Lapachone Scaffold: Novel Reagents for Reaction Profiling
Hatfield, M. Jason,Chen, Jingwen,Fratt, Ellie M.,Chi, Liying,Bollinger, John C.,Binder, Randall J.,Bowling, John,Hyatt, Janice L.,Scarborough, Jerrod,Jeffries, Cynthia,Potter, Philip M.
supporting information, p. 1568 - 1579 (2017/03/08)
Carboxylesterases (CEs) are ubiquitous enzymes that are responsible for the metabolism of xenobiotics, including drugs such as irinotecan and oseltamivir. Inhibition of CEs significantly modulates the efficacy of such agents. We report here that β-lapachone is a potent, reversible CE inhibitor with Ki values in the nanomolar range. A series of amino and phenoxy analogues have been synthesized, and although the former are very poor inhibitors, the latter compounds are highly effective in modulating CE activity. Our data demonstrate that tautomerism of the amino derivatives to the imino forms likely accounts for their loss in biological activity. A series of N-methylated amino derivatives, which are unable to undergo such tautomerism, were equal in potency to the phenoxy analogues and demonstrated selectivity for the liver enzyme hCE1. These specific inhibitors, which are active in cell culture models, will be exceptionally useful reagents for reaction profiling of esterified drugs in complex biological samples.
1,2- two alkone naphthalene compound and its preparation method and application
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Paragraph 0064; 0065, (2017/02/24)
The invention discloses a 1,2-diketone naphthalene compound which has a general structural formula (I) described in the specification, wherein Ar represents benzene ring, naphthalene ring, quinoline ring or isoquinoline ring, naphthalene diimide ring or coumarin ring; amino acid is directly connected with the Ar; when a substituent group exists on the Ar, R is an electron-withdrawing, electron-donating or neutral group. The invention further discloses a preparation method of the compound and application of the compound to preparation of inflammation-resistant and immunocompetence-resistant drugs. The compound is relatively good in inflammation and immunological competence resistance, is a CRAC (Ca release activated Ca) blocker with a novel structure, and can be used as a lead compound of the inflammation-resistant and immunocompetence-resistant drugs. According to the preparation method, the reaction condition is mild, raw materials are cheap and easily available, and the operation and the post-treatment process are simple.
HEAT SHOCK PROTEIN 90 INHIBITORS, METHODS OF PREPARING SAME, AND METHODS FOR THEIR USE
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Page/Page column 14, (2010/04/28)
Novel classes of molecular chaperone Heat shock protein 90 (Hsp90) inhibitors are disclosed. These compounds are useful in treating and preventing cancer and other Hsp90-related diseases and conditions, such as inflammation and neurodegenerative disorders. Methods of treating and preventing cancer and other Hsp90 related diseases and conditions are disclosed that include administering to the subject a therapeutically effective amount of an Hsp90 inhibitor. Methods of preparing the novel Hsp90 inhibitors are also provided.
