148550-51-0Relevant articles and documents
Synthesis and Evaluation of 2-Alkylthio-4-(N-substituted sulfonamide)pyrimidine Hydroxamic Acids as Anti-myeloma Agents
Xiang, Jinbao,Leung, Crystal,Zhang, Zhuoqi,Hu, Cassie,Geng, Chao,Liu, Lili,Yi, Lang,Li, Zhiwei,Berenson, James,Bai, Xu
, p. 472 - 477 (2016)
A series of pyrimidine hydroxamic acids with a sulfide substituent at the second position and a sulfonamide substituent at the fourth position have been synthesized and evaluated for their activity against human myeloma cell line RPMI 8226. Several compounds exhibited significant anti-cancer potency. It was found that representative compound 6a selectively killed cancerous but not normal cells. Moreover, compound 6a was effective in causing apoptosis in RPMI 8226 cells and exhibited promising HDAC-inhibitory activities.
Design, Synthesis, and Structure-Activity relationships of Evodiamine-Based topoisomerase (Top)/Histone deacetylase (HDAC) dual inhibitors
Dong, Guoqiang,Liang, Huixin,Liu, Dan,Meng, Xiangguo,Sheng, Chunquan,Wu, Shanchao,Zhu, Fugui
supporting information, (2022/03/16)
On the basis of synergistic effect between topoisomerase (Top) and histone deacetylase (HDAC) inhibitors, a series of novel evodiamine-based Top/HDAC dual inhibitors were designed and synthesized. Systematic structure?activity relationship (SAR) studies led to the discovery of compounds 29b and 45b, which simultaneously inhibited Top and HDAC and exhibited potent antitumor activities against the HCT116 cell line. Compounds 29b and 45b efficiently induced apoptosis with G2 cell cycle arrest and significantly inhibited cellular HDACs in HCT116 cells with good in vitro metabolic stabilities. Collectively, this work provides valuable SAR information and lead compounds for evodiamine-based Top/HDAC dual inhibitors.
Bicyclic Diazepinones as Dual Ligands of the α2δ-1 Subunit of Voltage-Gated Calcium Channels and the Norepinephrine Transporter
Díaz, José Luis,Cuevas, Félix,Pazos, Gonzalo,álvarez-Bercedo, Paula,Oliva, Ana I.,Sarmentero, M. ángeles,Font, Daniel,Jiménez-Aquino, Agustín,Morón, María,Port, Adriana,Pascual, Rosalía,Dordal, Albert,Portillo-Salido, Enrique,Reinoso, Raquel F.,Vela, José Miguel,Almansa, Carmen
, p. 2167 - 2185 (2021/03/09)
The synthesis and pharmacological activity of a new series of bicyclic diazepinones with dual activity toward the α2δ-1 subunit of voltage-gated calcium channels (Cavα2δ-1) and the norepinephrine transporter (NET) are reported. Exploration of the positions amenable for substitution on a nonaminoacidic Cavα2δ-1 scaffold allowed the identification of favorable positions for the attachment of NET pharmacophores. Among the patterns explored, attachment of the 2-ethylamino-9-methyl-6-phenyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one framework to the meta-position of the phenyl ring of the 3-methylamino-1-phenylpropoxy and 3-methylamino-1-thiophenylpropoxy moieties provided dual compounds with excellent NET functionality. Alternative bicyclic frameworks were also explored, and some lead molecules were identified, which showed a balanced dual profile and exhibited good ADMET properties.
Pyrimidine hydroxamicacid derivative and preparation method and application thereof
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Paragraph 0026; 0030; 0070; 0071, (2017/08/25)
The invention provides a pyrimidine hydroxamicacid derivativeshown as a general formula (I) and a preparation method and application thereof. The compound and its pharmaceutically acceptable salt can regulate an HDAC signal transduction pathway, increase the acetylated histone content in cells and selectively kill myeloma cells but have no obvious toxicity to normal human peripheral blood mononuclear cells. Therefore, the compound is expected to be developed into a safe anticancer drug.
PROCESS FOR THE SEPARATION OF ENANTIOMERS OF PIPERAZINE DERIVATIVES
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Page/Page column 51; 52, (2017/09/21)
The invention relates to a process for preparing either enantiomer of a compound of formula (I), wherein X, Y and n have the meaning given in claim 1, with high enantiomeric excess (e.e.), by chiral resolution in the presence of a non-racemic, chiral acid.
ACID ADDITION SALTS OF PIPERAZINE DERIVATIVES
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Page/Page column 87, (2017/09/09)
The invention relates to acid addition salts of piperazine derivatives, as well as solid forms, such as polymorphic forms, thereof, which are useful as pharmaceutical ingredients and in particular as glycosidase inhibitors.
SUBSTITUTED BICYCLIC HETEROARYL COMPOUNDS AS RXR AGONISTS
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Paragraph 0386, (2016/12/01)
The present invention relates to certain substituted bicyclic compounds that are agonists of RXR and which are therefore useful in the treatment of certain disorders that can be prevented or treated by activation of this receptor. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders.
GLYCOSIDASE INHIBITORS
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Page/Page column 155, (2016/03/22)
Compounds of formula (I) wherein A, R, W, Q, n and m have the meaning according to the claims can be employed, inter alia, for the treatment of tauopathies and Alzheimer's disease.
DERIVATIVES OF 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOLS AS PHOSPHODIESTERASE INHIBITORS
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Paragraph 1022; 1023, (2013/04/10)
The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
DERIVATIVES OF 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOLS AS PHOSPHODIESTERASE INHIBITORS
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, (2013/04/13)
The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
