91367-05-4Relevant articles and documents
Design, synthesis and evaluation of novel 2-(1H-imidazol-2-yl) pyridine Sorafenib derivatives as potential BRAF inhibitors and anti-tumor agents
Jiao, Yu,Xin, Bo-Tao,Zhang, Yanmin,Wu, Jianbing,Lu, Xiaolin,Zheng, Ying,Tang, Weifang,Zhou, Xiang
, p. 170 - 183 (2015/01/08)
A series of 2-(1H-imidazol-2-yl) pyridine derivatives (CLW01-CLW31) have been designed and synthesized, and they were screened for BRAF kinase inhibitory activity. Besides, their biological activities were evaluated in vitro and in vivo. All the compounds were reported for the first time, and compounds CLW14 and CLW27 displayed the most potent antiproliferative activity against cell line A375 in vitro, with IC50 values of 4.26 and 2.93 1/4M, respectively, which were comparable with the positive control Sorafenib. Those two compounds were further evaluated for the in vivo efficacy using an A375 xenograft nude mice model. The results showed that the growth of A375 cancer cells xenografts was suppressed by factors of 35.68% and 42.50% (percent tumor growth inhibition values) after intragastric (ig) administration of compound CLW14 and CLW27 at concentration of 50 mg/kg. Thus they may be promising lead compounds to be developed as an alternative for current Sorafenib therapy.
5-ALKYLOXY-INDOLIN-2-ONE DERIVATIVES, PREPARATION THEREOF AND APPLICATION THEREOF IN THERAPY
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Page/Page column 9-10, (2010/04/23)
The present invention relates to derivatives of 5-alkyloxy-indolin-2-one, their method of production and their therapeutic applications. These novel derivatives have affinity and selectivity for the V2 receptors of vasopressin (“V2 receptors”) and can therefore constitute active principles of pharmaceutical compositions.
Design, synthesis and identification of novel colchicine-derived immunosuppressant
Chang, Dong-Jo,Yoon, Eun-Young,Lee, Geon-Bong,Kim, Soon-Ok,Kim, Wan-Joo,Kim, Young-Myeong,Jung, Jong-Wha,An, Hongchan,Suh, Young-Ger
scheme or table, p. 4416 - 4420 (2010/04/05)
Synthesis and biological evaluation of various colchicine analogues through the mixed-lymphocyte reaction (MLR), lymphoproliferation, and inhibitory effects on the inflammatory genes are described. In addition, a new series of immunosuppressive agents developed on the structural basis of colchicine, as well as their structure-activity relationships is reported. The most potent analogue 20a exhibited an excellent immunosuppressive activity on in vivo skin-allograft model, which is comparable to that of cyclosporin A.
DIARYL ACETIC ACID DERIVATIVES AND THE PREPARATION THEREOF
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Page/Page column 6, (2008/06/13)
The invention relates to compounds of the general formula (I), wherein R stands for nitro group or -COOR1 group, wherein R1 stands for hydrogen atom or for C1-4 straight or branched alkyl group, R2 stands for hy