Discovery of Phthalimides as Immunomodulatory and Antitumor Drug Prototypes
作者:Claudia Pessoa、Paulo Michel P. Ferreira、Letícia Veras C. Lotufo、Manoel O. de Moraes、Suellen M. T. Cavalcanti、Lucas Cunha D. Coêlho、Marcelo Z. Hernandes、Ana Cristina L. Leite、Carlos A. De Simone、Vlaudia M. A. Costa、Valdênia M. O. Souza
DOI:10.1002/cmdc.200900525
日期:2010.4.6
Optimized anticancer agents: A set of functionalized phthalimides was synthesized and evaluated for antitumor activities and as modulators of the secretion of cytokines and nitric oxide. Their potency was compared with that of thalidomide, and as a result, a new potent anticancer and immunomodulatory agent, compound 2 b, was identified.
[EN] TRIAZOLOTRIAZINE DERIVATIVES AS A2A RECEPTOR ANTAGONISTS<br/>[FR] DÉRIVÉS DE TRIAZOLOTRIAZINE EN TANT QU'ANTAGONISTES DU RÉCEPTEUR A2A
申请人:ZHEJIANG VIMGREEN PHARMACEUTICALS LTD
公开号:WO2020002969A1
公开(公告)日:2020-01-02
The present invention provides triazolotriazine derivatives of formula (1) as A2A receptor antagonists. Compounds of formula (1) and pharmaceutical compositions including the compounds can be used for the treatment of disorders related to A2A receptor hyperfunctioning, such as certain types cancers. Compounds of formula (1) and methods of preparing the compounds are disclosed in the invention.
Microscale Parallel Synthesis of Acylated Aminotriazoles Enabling the Development of Factor XIIa and Thrombin Inhibitors
作者:Simon Platte、Marvin Korff、Lukas Imberg、Ilker Balicioglu、Catharina Erbacher、Jonas M. Will、Constantin G. Daniliuc、Uwe Karst、Dmitrii V. Kalinin
DOI:10.1002/cmdc.202100431
日期:2021.12.14
approach toward N-acylated aminotriazoles is reported, enabling the compounds’ screening against FXIIa and thrombin. This approach afforded low-nanomolar FXIIa and thrombininhibitors with no off-targeting of the other tested serine proteases. Selected compounds were shown to be covalent inhibitors of FXIIa and demonstrated anticoagulant properties in vitro, influencing the intrinsic blood coagulation
Fenbufen, a New Anti-Inflammatory Analgesic: Synthesis and Structure-Activity Relationships of Analogs
作者:Ralph G. Child、Arnold C. Osterberg、Adolph E. Sloboda、Andrew S. Tomcufcik
DOI:10.1002/jps.2600660403
日期:1977.4
hundred analogs of fenbufen were prepared and tested using the carrageenan, polyarthritis, and UV erythema anti-inflammatory tests and the 2-phenyl-1,4-benzoquinone writhing and inflamed paw pressure analgesic tests. Only three retained the same full spectrum of activity as fenbufen: dl-4-(4-biphenylyl)-4-hydroxybutyric acid, dl-4-(4-biphenylyl)-1,4-butanediol, and 4-biphenylacetic acid. Fenbufen had the
two-fold excess of amines and ultrasonic influence increased yield of target products and reduced reaction time. The structures of the products were proved by two-dimensional correlation spectra of HSQC, HMBC, COSY, NOESY. A new efficient method for the synthesis of a large group of hybrid potentially biologically active compounds by condensation of methyl maleopimarate with various amines (glycine, β-alanine