854382-06-2Relevant academic research and scientific papers
Towards new sila- Or germa-derivatives of motesanib
Boddaert, Thomas,Querolle, Olivier,Meerpoel, Lieven,Angibaud, Patrick,Maddaluno, Jacques,Durandetti, Muriel
, p. 1210 - 1218 (2019/07/31)
– Developing new access to original silylated heterocycles is an emerging challenge in medicinal chemistry. In this paper, we describe a synthesis of silylated and germylated Motesanib analogues relying on a peptide coupling between a nicotinic acid derivative and silylated or germylated heterocycles, prepared according to our previous reports.
Exploration of 2-((Pyridin-4-ylmethyl)amino)nicotinamide Derivatives as Potent Reversal Agents against P-Glycoprotein-Mediated Multidrug Resistance
Qiu, Qianqian,Shi, Wei,Li, Zheng,Zhang, Bo,Pan, Miaobo,Cui, Jian,Dai, Yuxuan,Huang, Wenlong,Qian, Hai
, p. 2930 - 2943 (2017/04/21)
Overexpression of the ATP-binding cassette (ABC) transport proteins, like ABCB1, commonly referred to as P-glycoprotein (P-gp), initiates active efflux of a broad spectrum of unrelated chemotherapeutic drugs in structure and function, leading to chemotherapy failure. A series of 2-((pyridin-4-ylmethyl)amino)nicotinamide derivatives as potent reversal agents against P-glycoprotein-mediated multidrug resistance (MDR) were designed and synthesized. The majority of target compounds displayed great reversal potency, especially 9n. In-depth studies demonstrated 9n has high potency (EC50 = 119.6 ± 6.9 nM), low cytotoxicity, and long duration (>24 h) in reversing adriamycin (ADM) resistance in K562/A02 cells. 9n also improved the effects of other cytotoxic agents related to MDR, increased accumulation of ADM, interrupted P-gp-mediated Rh123 efflux function, and suppressed P-gp ATPase activity in K562/A02 MDR cells. The Western blot analysis indicated that the MDR reversal by 9n was not due to a decrease in protein expression. Besides, the effect of CYP3A4 was not influenced by 9n, avoiding the toxicity caused by drug interactions. The study yielded 9n with superior properties compared to the classical inhibitor verapamil (VRP) and leading compound apatinib.
2 - aminomethyl pyridine-based nicotinamide compound and its preparation method and application (by machine translation)
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Paragraph 0082-0086, (2017/08/28)
The invention relates to the general formula (I) compounds and salts thereof, such compounds have a strong reverse tumor multi-drug resistance (MDR) function, activity is far higher than the veraparnil, and has a small cell toxicity, the invention also re
Discovery of N-phenyl nicotinamides as potent inhibitors of Kdr
Dominguez, Celia,Smith, Leon,Huang, Qi,Yuan, Chester,Ouyang, Xiaohu,Cai, Lynn,Chen, Paul,Kim, Joseph,Harvey, Timothy,Syed, Rashid,Kim, Tae-Seong,Tasker, Andrew,Wang, Ling,Zhang, Michael,Coxon, Angela,Bready, James,Starnes, Charles,Chen, Danlin,Gan, Yongmei,Neervannan, Sesha,Kumar, Gondi,Polverino, Anthony,Kendall, Richard
, p. 6003 - 6008 (2008/03/11)
Inhibition of tumor-induced angiogenesis is a promising strategy in anticancer research. Neovascularization is a process required for both tumor growth and metastasis. Enhanced understanding of the underlying molecular mechanisms has led to the discovery
