274673-37-9Relevant academic research and scientific papers
De novo design, synthesis and evaluation of benzylpiperazine derivatives as highly selective binders of Mcl-1
Ding, Xiao,Li, Yan,Lv, Li,Zhou, Mi,Han, Li,Zhang, Zhengxi,Ba, Qian,Li, Jingquan,Wang, Hui,Liu, Hong,Wang, Renxiao
, p. 1986 - 2014 (2014/01/06)
Considerable efforts have been made to the development of small-molecule inhibitors of antiapoptotic B-cell lymphoma 2 (Bcl-2) family proteins (such as Bcl-2, Bcl-xL, and Mcl-1) as a new class of anticancer therapies. Unlike general inhibitors
PROCASPASE-ACTIVATING COMPOUNDS AND COMPOSITIONS
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Paragraph 0088; 0123-0124, (2013/04/24)
The invention provides compounds and compositions useful for the modulation of certain enzymes. The compounds and compositions can induce of cell death, particularly cancer cell death. The invention also provides methods for the synthesis and use of the compounds and compositions, including the use of compounds and compositions in therapy for the treatment of cancer and selective induction of apoptosis in cells.
COMPOUNDS FOR TREATING CANCER
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Page/Page column 37, (2010/07/02)
Compounds of general formula (I): wherein R1, R2, R3, R4, R5, R6, X and Y are as defined herein are inhibitors of Bcl-2 and are useful for treating diseases characterised by abnormal cell growth and/or dysregulated apoptosis.
Characterization of tunable piperidine and piperazine carbamates as inhibitors of endocannabinoid hydrolases
Long, Jonathan Z.,Jin, Xin,Adibekian, Alexander,Li, Weiwei,Cravatt, Benjamin F.
experimental part, p. 1830 - 1842 (2010/08/19)
Monoacylglycerol lipase (MAGL) and fatty acid amide hydrolase (FAAH) are two enzymes from the serine hydrolase superfamily that degrade the endocannabinoids 2-arachidonoylglycerol and, anandamide, respectively. We have recently discovered that, MAGL and, FAAH are both inhibited by carbamates bearing an N-piperidine/piperazine group. Piperidine/piperazine carbamates show excellent in vivo activity, raising brain endocannabinoid levels and producing CB1-dependent behavioral effects in mice, suggesting that they represent a promising class of inhibitors for studying the endogenous functions of MAGL and FAAH. Herein, we disclose a full account of the syntheses, structure-activity relationships, and, inhibitory activities of piperidine/piperazine carbamates against members of the serine hydrolase family. These scaffolds can be tuned for MAGL-selective or dual MAGL-FAAH inhibition by the attachment of an, appropriately substituted bisarylcarbinol or aryloxybenzyl moiety, respectively, on the piperidine/piperazine ring. Modifications to the piperidine/piperazine ring ablated inhibitory activity, suggesting a strict requirement for a six-membered ring to maintain potency.
