205643-03-4Relevant academic research and scientific papers
Palladium-Catalyzed C-H/C-H Cross-Coupling by Mechanochemistry: Direct Alkenylation and Heteroarylation of N1-Protected 1 H-Indazoles
Yu, Jingbo,Yang, Xinjie,Wu, Chongyang,Su, Weike
, p. 1009 - 1021 (2020/01/09)
C3-alkenylated and C3-(hetero)arylated 1H-indazoles are privileged structural motifs in numerous pharmaceuticals. Direct C3-alkenylation and C3-(hetero)arylation of 1H-indazoles have been significantly challenging because of the inert nature of this carbon center. Herein, we present an efficient mechanochemical strategy for palladium-catalyzed C-H/C-H cross-coupling to construct C3-alkenylated and C3-heteroarylated 1H-indazoles using low-cost copper oxidants with satisfactory product yields and broad functional group tolerance. The robustness of the developed protocols was further demonstrated by the unprecedented total mechanosynthesis of the intermediate of PLK4 inhibitor CFI-400945 and HIF-1α inhibitor YC-1.
Hypoxia-Targeting Organometallic Ru(II)-Arene Complexes with Enhanced Anticancer Activity in Hypoxic Cancer Cells
Zhao, Jian,Li, Wanchun,Gou, Shaohua,Li, Shuang,Lin, Shengqiu,Wei, Qianhui,Xu, Gang
, p. 8396 - 8403 (2018/07/25)
As hypoxia is an important factor to limit chemotherapeutic efficacy in tumors, we herein report three ruthenium(II)-arene complexes containing a hypoxia inducible factor-1α inhibitor (YC-1), which endow the organometallic complexes with potential for hyp
Preparation method of indazole and application of indazole in medicine synthesis
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, (2017/04/21)
The invention belongs to the field of chemicals, and relates to a preparation method of indazole and an application of the indazole in medicine synthesis. The invention discloses a preparation method of indazole and an application of the indazole in synthesizing 1H-indazole-3-carboxylic acid, lonidamine, a compound 8, a compound 9, a compound 10, axitinib, YD-3, YC-1 and similar substances thereof.
Copper(I) Oxide-Mediated Cyclization of o-Haloaryl N-Tosylhydrazones: Efficient Synthesis of Indazoles
Tang, Meng,Kong, Yuanfang,Chu, Bingjie,Feng, Dan
, p. 926 - 939 (2016/04/05)
An efficient synthesis of indazoles from readily accessible E/Z mixtures of o-haloaryl N-tosylhydrazones has been developed. The thermo-induced isomerization of N-tosylhydrazones is discussed. A series of valuable indazole derivatives are prepared in good yields, and the method has been successfully applied to the synthesis of the bioactive compounds, lonidamine, AF-2785, axitinib, YC-1 and YD-3.
Novel Pyrazole Derivatives Effectively Inhibit Osteoclastogenesis, a Potential Target for Treating Osteoporosis
Kuo, Ting-Hao,Lin, Tzu-Hung,Yang, Rong-Sen,Kuo, Sheng-Chu,Fu, Wen-Mei,Hung, Hsin-Yi
, p. 4954 - 4963 (2015/07/02)
As human beings live longer, age-related diseases such as osteoporosis will become more prevalent. Intolerant side effects and poor responses to current treatments are observed. Therefore, novel effective therapeutic agents are greatly needed. Here, pyrazole derivatives were designed and synthesized, and their osteoclastogenesis inhibitory effects both in vitro and in vivo were evaluated. The most promising compound 13 with a 2-(dimethylamino)ethyl group inhibited markedly in vitro osteoclastogenesis as well as the bone resorption activity of osteoclasts. Compound 13 affected osteoclasts early proliferation and differentiation more than later fusion and maturation stages. In ovariectomized (OVX) mice, compound 13 can inhibit the loss of trabecular bone volume, trabecular bone number, and trabecular thickness. Moreover, compound 13 can antagonize OVX-induced reduction of serum bone resorption marker and then compensatory increase of the bone formation marker. To sum up, compound 13 has high potential to be developed into a novel therapeutic agent for treating osteoporosis in the future.
The design, synthesis, and biological evaluation of novel YC-1 derivatives as potent anti-hepatic fibrosis agents
Xiao, Juan,Jin, Chunmei,Liu, Zhixue,Guo, Shujing,Zhang, Xiaochuan,Zhou, Xin,Wu, Xue
, p. 7257 - 7264 (2015/07/01)
1-Benzyl-3-(substituted aryl)-5-methylfuro[3,2-c]pyrazole (YC-1) is a well-known synthetic compound with various satisfactory pharmacological activities, such as the activation of soluble guanylate cyclase (sGC) and the inhibition of hypoxia-induced facto
Design, synthesis and insight into the structure-activity relationship of 1,3-disubstituted indazoles as novel HIF-1 inhibitors
An, Hongchan,Kim, Nam-Jung,Jung, Jong-Wha,Jang, Hannah,Park, Jong-Wan,Suh, Young-Ger
scheme or table, p. 6297 - 6300 (2011/11/29)
Design, synthesis and insight into the structure-activity relationship (SAR) of 1,3-disubstituted indazoles as novel HIF-1 inhibitors are described. In particular, the substituted furan moiety on indazole skeleton as well as its substitution pattern turns
ANTI-ANGIOGENESIS COMPOUNDS
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Page/Page column 126, (2010/11/27)
The present invention provides methods and pharmaceutical compositions for inhibiting expressions of HIF and HIF regulated genes, inhibiting angiogenesis, inducing cell cycle arrest in tumor cells, and treating cell proliferating diseases or conditions
COMPOUNDS, COMPOSITIONS AND METHODS
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, (2008/06/13)
The present invention provides methods and pharmaceutical compositions for inhibiting expressions of HIF and HIF regulated genes, inhibiting angiogenesis, inducing cell cycle arrest in tumor cells, and treating cell proliferating diseases or conditions.
Blockade of voltage dependent sodium channels
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, (2008/06/13)
Compounds of formula (1), and pharmaceutically acceptable salts thereof, are capable of blockading voltage-dependent sodium channels and are useful in particular, in treating glaucoma and multiple sclerosis.
