1572-01-6Relevant academic research and scientific papers
COMPOUNDS FOR TREATING TUBERCULOSIS
-
, (2021/06/04)
The invention concerns a compound of formula (Ia) or (Ib) wherein R1 is hydrogen or a methyl group; R2 is an unsubstituted or substituted alkyl group; R3 is an aryl group or a heteroaryl group, optionally substituted by on
Novel imidazole derivatives having FLT3-inhibitory activity and use thereof
-
Paragraph 0338-0341; 0356-0358, (2020/04/22)
The present invention relates to a novel benzoimidazole derivative having fms-like tyrosine kinase 3 (FLT3) inhibitory activity, and a use thereof. The novel benzoimidazole derivative or a pharmaceutically acceptable salt thereof according to the present invention exhibits excellent inhibitory activity on FLT3, thereby being expected for target treatment through further fundamental approach in preventing or treating acute myeloid leukemia (AML).COPYRIGHT KIPO 2020
Design, synthesis and in vitro evaluation of 6-amide-2-aryl benzoxazole/benzimidazole derivatives against tumor cells by inhibiting VEGFR-2 kinase
Yuan, Xu,Yang, Qingyi,Liu, Tongyan,Li, Ke,Liu, Yuwen,Zhu, Changcheng,Zhang, Zhiyun,Li, Linghua,Zhang, Conghai,Xie, Mingjin,Lin, Jun,Zhang, Jihong,Jin, Yi
, p. 147 - 165 (2019/06/27)
Herein, we have carried out a structural optimization campaign to discover the novel anti-tumor agents with our previously screened YQY-26 as the hit compound. A library of thirty-seven 6-amide-2-aryl benzoxazole/benzimidazole derivatives has been designe
Discovery of 6-Arylurea-2-arylbenzoxazole and 6-Arylurea-2-arylbenzimidazole Derivatives as Angiogenesis Inhibitors: Design, Synthesis and in vitro Biological Evaluation
Zi, Mengli,Liu, Feifei,Wu, Di,Li, Ke,Zhang, Da,Zhu, Changcheng,Zhang, Zhiyun,Li, Linghua,Zhang, Conghai,Xie, Mingjin,Lin, Jun,Zhang, Jihong,Jin, Yi
, p. 1291 - 1302 (2019/06/27)
We embarked on a structural optimization campaign aimed at the discovery of novel anti-angiogenesis agents with previously reported imidazole kinase inhibitors as a lead compound. A library of 29 compounds was synthesized. Several title compounds exhibite
Discovery of N-(2-phenyl-1H-benzo[d]imidazol-5-yl)quinolin-4-amine derivatives as novel VEGFR-2 kinase inhibitors
Shi, Lei,Wu, Ting-Ting,Wang, Zhi,Xue, Jia-Yu,Xu, Yun-Gen
, p. 698 - 707 (2014/08/18)
Inhibition of the VEGF signaling pathway has become a valuable approach in the treatment of cancers. In this work, a series of N-(2-phenyl-1H-benzo[d]imidazol-5-yl)quinolin-4-amine derivatives were designed and identified as potent inhibitors of VEGFR-2 (
Discovery of quinazolin-4-amines bearing benzimidazole fragments as dual inhibitors of c-Met and VEGFR-2
Shi, Lei,Wu, Ting-Ting,Wang, Zhi,Xue, Jia-Yu,Xu, Yun-Gen
, p. 4735 - 4744 (2014/10/15)
Both c-Met and VEGFR-2 are important targets for the treatment of cancers. In this study, a series of N-(2-phenyl-1H-benzo[d]imidazol-5-yl)quinazolin-4- amine derivatives were designed and identified as dual c-Met and VEGFR-2 inhibitors. Among these compounds bearing quinazoline and benzimidazole fragments, compound 7j exhibited the most potent inhibitory activity against c-Met and VEGFR-2 with IC50 of 0.05 μM and 0.02 μM, respectively. It also showed the highest anticancer activity against the tested cancer cell lines with IC50 of 1.5 μM against MCF-7 and 8.7 μM against Hep-G2. Docking simulation supported the initial pharmacophoric hypothesis and suggested a common mode of interaction at the ATP-binding site of c-Met and VEGFR-2, which demonstrates that compound 7j is a potential agent for cancer therapy deserving further researching.
Discovery of 2-arylbenzoxazoles as upregulators of utrophin production for the treatment of duchenne muscular dystrophy
Chancellor, Daniel R.,Davies, Kay E.,De Moor, Olivier,Dorgan, Colin R.,Johnson, Peter D.,Lambert, Adam G.,Lawrence, Daniel,Lecci, Cristina,Maillol, Carole,Middleton, Penny J.,Nugent, Gary,Poignant, Séverine D.,Potter, Allyson C.,Price, Paul D.,Pye, Richard J.,Storer, Richard,Tinsley, Jonathon M.,Van Well, Renate,Vickers, Richard,Vile, Julia,Wilkes, Fraser J.,Wilson, Francis X.,Wren, Stephen P.,Wynne, Graham M.
, p. 3241 - 3250 (2011/07/06)
Figure Presented. A series of novel 2-arylbenzoxazoles that upregulate the production of utrophin in murine H2K cells, as assessed using a luciferase reporter linked assay, have been identified. This compound class appears to hold considerable promise as a potential treatment for Duchenne muscular dystrophy. Following the delineation of structure-activity relationships in the series, a number of potent upregulators were identified, and preliminary ADME evaluation is described. These studies have resulted in the identification of 1, a compound that has been progressed to clinical trials.
