852233-77-3Relevant academic research and scientific papers
Toward a novel class of antithrombotic compounds with dual function. Discovery of 1,4-benzoxazin-3(4H)-one derivatives possessing thrombin inhibitory and fibrinogen receptor antagonistic activities
Anderluh, Petra ?tefani?,Anderluh, Marko,Ila?, Janez,Mravljak, Janez,Dolenc, Marija Sollner,Stegnar, Mojca,Kikelj, Danijel
, p. 3110 - 3113 (2005)
A novel class of potential antithrombotic compounds with moderate thrombin inhibitory and fibrinogen receptor antagonistic activity is described. Combination of anticoagulant and antiaggregatory activity in the same molecular entity is presented as a new
Design, synthesis and antitumor assessment of phenylureas bearing 5-fluoroindolin-2-one moiety
Cai, Yunrui,Chen, Tong,Zhu, Huajian,Zou, Hongbin
, p. 958 - 968 (2020/08/19)
Background: The development of novel antineoplastic agents remains highly desirable. Objective: This study focuses on the design, synthesis, and antitumor evaluation of phenyl ureas bearing 5-fluoroindolin-2-one moiety. Methods: Three sets of phenylureas were designed and synthesized and their antiproliferative abil-ity was measured against four human carcinoma cell lines (Hela, Eca-109, A549, and MCF-7) via MTT assay. In vivo anticancer activity was further evaluated in xenograft models of human breast cancer (MCF-7). Results: A total of twenty-one new compounds were synthesized and characterized by means of1 H and13 C NMR as well as HR-MS. Three sets of compounds (1a?1c, 2a?2c, and 3a?3c) were ini-tially constructed, and preliminary antiproliferative activities of these molecules were evaluated against Hela, Eca-109, A549 and MCF-7, highlighting the meta-substituted phenylureas (1a?1c) as the most cytotoxic set. A series of meta-substituted phenylureas derivatives (1d?1o) were then designed and synthesized for structure-activity relationship study. Most of the new compounds showed desirable cytotoxicity, among which compound 1g exhibited the most remarkable cyto-toxic effects against the tested human cancer cells with IC50 values ranging from 1.47 to 6.79 μM. Further studies showed that compound 1g suppressed tumor growth in human breast cancer (MCF-7) xenograft models without affecting the body weight of its recipients. Conclusion: In this study, twenty-one new compounds, containing the privileged structures of phenylurea and 5-fluoroindolin-2-one, were designed and synthesized. Subsequent structure-activity studies showed that 1g was the most bioactive antitumor agent among all tested com-pounds, hence a potentially promising lead compound once given further optimization.
5-Quinoline derivatives having an anti-bacterial activity
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Page/Page column 18, (2010/12/31)
The present invention describes novel anti-bacterial compounds of the formula (I). These compounds are, amongst others, of interest as inhibitors of DNA gyrase and topoisomerases, for example of topoisomerase II and IV.
ANTITHROMBOTIC COMPOUNDS WITH DUAL FUNCTION
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Page/Page column 36-38, (2010/02/11)
The present invention comprises compounds of the general formula (I) : and pharmaceutically acceptable salts thereof, wherein the substituents have in the description specified meaning. The compounds are used as antithrombotic agents possessing inhibitory
