905986-89-2Relevant academic research and scientific papers
Synthesis and Evaluation of Anti-inflammatory N-Substituted 3,5-Bis(2-(trifluoromethyl)benzylidene)piperidin-4-ones
Xie, Zixin,Zhang, Zaikui,Yu, Shufang,Cheng, Donghua,Zhang, Huan,Han, Chao,Lv, Handeng,Ye, Faqing
, p. 327 - 336 (2017/03/01)
A total of 24 N-substituted 3,5-bis(2-(trifluoromethyl)benzylidene)piperidin-4-one derivatives were synthesized via aldol condensation, and their anti-inflammatory activities were evaluated. These compounds were found to have no significant cytotoxicity a
Novel 2H-pyrazolo[4,3-c]hexahydropyridine derivatives: Synthesis, crystal structure, fluorescence properties and cytotoxicity evaluation against human breast cancer cells
Pang, Chuncheng,Sun, Chuanwen,Wang, Jing,Xiao, Di,Ding, Li,Bu, Hongfei
, p. 702 - 715 (2013/07/19)
A series of novel 2H-pyrazolo[4,3-c]hexahydropyridine derivatives (II) have been designed and synthesized. The target compounds have been identified by elemental analysis and spectral (1H NMR, IR, and MS) data and the absolute configuration of compound (II 1 ) was confirmed by single crystal X-ray diffraction. The cytotoxicity of the target compounds have been evaluated in vitro against two human breast cancer cell lines MCF-7 and MDA-MB-231 by MTT assay. Most compounds exhibited good inhibition, and compounds II 21 (IC50 = 4.7 μM for MCF-7 and IC50 = 9.3 μM for MDA-MB-231), II 33 (IC50 = 2.4 μM for MCF-7 and IC50 = 4.2 μM for MDA-MB-231) and II 40 (IC50 = 3.3 μM for MCF-7 and IC50 =8.6 μM for MDA-MB-231) displayed better inhibitory activity than 5-fluorouracil (IC 50 = 4.8 μM for MCF-7 and IC50 = 9.6 μM for MDA-MB-231, respectively). Flow cytometric analysis and DNA fragmentation suggest that II 33 is cytotoxic and able to induce the apoptosis of MCF-7 cells. The fluorescence properties of compounds II 1, II 6, II 11, II 16, II 23, II 28, and II 35 were also studied and compound II 28 afforded the highest photoluminescence quantum yield (38%).
Synthesis, crystal structure and anticancer activities of tetrahydropyrido[4,3-d]dihydropyrimidine-2-thiones
Ding, Li,Xue, Sijia,Li, Jing,Xiao, Di,Wang, Jing,Hao, Zhibing,Pang, Chuncheng
, p. 2509 - 2516 (2013/01/15)
A new series of tetrahydropyrido[4,3-d]dihydropyrimidine-2-thiones (3a-3x) were designed and synthesized. Their structures were confirmed by1H NMR, IR, MS and elemental analysis, and the conformation of compound 3j was confirmed by X-ray diffraction. Preliminary bioassays indicated that most of the target compounds presented good antiproliferative activities against leukemic K562 cells, ovarian cancer HO-8910 cells and liver cancer SMMC-7721 cells in vitro. Among them the compounds 3i and 3m afford the best activity, the IC 50 of them were 3.22 and 3.65 iμg/mL against leukemic K562 cells, respectively, which were lower than the anticancer drug of clinical practice 5-FU (IC50=8.56 iμg/mL). Preliminary mechanism of action studies revealed that compound 3i caused DNA fragmentation and activated caspase-3/7 in leukemic K562 cells. A new series of tetrahydropyrido[4,3-d] dihydropyrimidine-2-thiones (3a-3x) were synthesized and the conformation of compound 3j was confirmed by X-ray diffraction. Preliminary bioassays indicated that most of the target compounds presented good antiproliferative activities against leukemic K562 cells, ovarian cancer HO-8910 cells and liver cancer SMMC-7721 cells in vitro. Preliminary mechanism of action studies revealed that compound 3i caused DNA fragmentation and activated caspase-3/7 in leukemic K562 cells. Copyright
Synthesis of N1 -alkyl-1,4-diazepin-5-ones via Schmidt ring expansion chemistry
Frick, Morin,McAtee, Danielle,McAtee, Jesse,Wysoczynski, Christina,Ray, Partha S.
experimental part, p. 17 - 19 (2011/10/02)
Reaction of 4-piperidone with alkyl bromides gave the corresponding N-alkyl-4-piperidones, and treatment of these with hydrazoic acid resulted in the Schmidt reaction to give the corresponding N1-alkyl-1,4-diazepin- 5-ones in good overall yield
N-(substituted benzyl)-3,5-bis(benzylidene)-4-piperidones: Synthesis and preliminary anti-leukemia activity (I)
Wang, Jing,Meng, Wen,Ni, Zhenjie,Xue, Sijia
, p. 2109 - 2113 (2012/03/11)
A series of novel N-(substituted benzyl)-3,5-bis(benzylidene)-4-piperidones 5a-5o were synthesized with substituted benzylamines as raw materials via a series of Michael addition, Dieckmann condensation, hydrolysis decarboxylation and aldol condensation.
Synthesis and structure-activity relationships of spirohydantoin-derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1)
Rowbottom, Martin W.,Vickers, Troy D.,Tamiya, Junko,Zhang, Mingzhu,Dyck, Brian,Grey, Jonathan,Schwarz, David,Heise, Christopher E.,Hedrick, Michael,Wen, Jenny,Tang, Hui,Wang, Hua,Fisher, Andrew,Aparicio, Anna,Saunders, John,Goodfellow, Val S.
, p. 2171 - 2178 (2007/10/03)
The design, synthesis, and SAR of a series of substituted spirohydantoins are described. Optimization of an in-house screening hit gave compounds that exhibited potent binding affinity and functional activity at MCH-R1.
PESTICIDAL SUBSTITUTED PIPERIDINES
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Page/Page column 51, (2008/06/13)
The invention relates to the use of piperidine derivatives encompassed from the general formula (I) for the control of pests, including arthropods and helminths, and a method for the control of pests.
