- Sophoridine pyrrole, indole derivative and preparation method and application thereof
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The invention relates to a sophoridine pyrrole, indole derivative. The invention discloses a chemical structure of the compound and further discloses a preparation method of the compound. In vitro anti-tumor activity researches show that anti-tumor drugs
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Paragraph 0191; 0193; 0196; 0202
(2018/09/08)
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- Design, synthesis, biological evaluation and structure-activity relationship of sophoridine derivatives bearing pyrrole or indole scaffold as potential antitumor agents
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Taking sophoridine as a lead compound, 58 sophoridine derivatives were designed, synthesized and evaluated for their antiproliferative activity in the HepG2 cancer cell line. Among the 58 compounds, 33 compounds showed potent antiproliferative activity wi
- Li, Zheng,Luo, Mengyang,Cai, Bin,Haroon-Ur-Rashid,Huang, Mengtian,Jiang, Jun,Wang, Lisheng,Wu, Lichuan
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p. 665 - 682
(2018/08/23)
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- Discovery of novel 3-benzylquinazolin-4(3H)-ones as potent vasodilative agents
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In the present study, a series of 3-benzylquinazolin-4(3H)-ones were synthesized and characterized. Their vasodilative effects were evaluated by wire myograph on isolated rat mesenteric arterial ring induced contraction with 60 mM KCl. The SAR of target compounds was discussed preliminarily. Among these compounds, 2a and 2c displayed potent vasodilatation action and could compete significantly the rat mesenteric arterial rings induced contraction with phenylephrine. Compounds 2a and 2c were further tested for their antihypertensive effects in SHR by oral administration. The results indicated that 2a and 2c could reduce significantly both diastolic and systolic blood pressure. Moreover, 2c displayed antihypertensive effect in a dose dependent manner, and could maintain the effects for 6 h at a dosage of 4.0 mg/kg. These findings suggest that the title compounds are novel vasodilative agents, representing a novel series of promising antihypertensive agents.
- Zuo, Sai-Jie,Li, Sen,Yu, Rui-Hong,Zheng, Guo-Xun,Cao, Yong-Xiao,Zhang, San-Qi
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p. 5597 - 5601
(2015/01/08)
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- Discovery of highly potent and selective benzyloxybenzyl-based peroxisome proliferator-activator receptor (PPAR) δ agonists
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A series of 1,4-benzyloxybenzylsulfanylaryl carboxylic acids were prepared and their activities for PPAR receptor subtypes (α, δ, and γ) with potential indications for the treatment of dyslipidemia were investigated. Analog 13a displayed the greatest binding affinity (IC50 = 10 nM) and selectivity (120-fold) for PPARδ over PPARα. Many of the analogs investigated were found to be highly selective for PPARδ and were dependent on the point of attachment of the substituent. In the 1,4-series, analog 28e was found to be the most potent (IC50 = 1.7 nM) and selective (>1000-fold) compound for PPARδ. None of the compounds tested showed appreciable binding affinity for PPARγ.
- Bratton, Larry D.,Filzen, Gary F.,Geyer, Andrew,Hoffman, Jennifer K.,Lu, Gina,Pulaski, Jim,Trivedi, Bharat K.,Unangst, Paul C.,Xu, Xiangyang
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p. 3624 - 3629
(2008/02/13)
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- Compounds that modulate PPAR activity and methods for their preparation
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This invention discloses compounds that alter PPAR activity. The invention also discloses pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing disipidemia, hypercholesteremia, obesity, eating disorders, hyperglycemia, atherosclerosis, hypertriglyceridemia, hyperinsulinemia and diabetes in a mammal as well as methods of supressing appetite and modulating leptin levels in a mammal. The present invention also discloses methods for making the disclosed compounds.
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