Synthesis and Biological Evaluation of 9-Oxo-9H-indeno[1,2-b]pyrazine-2,3-dicarbonitrile Analogues as Potential Inhibitors of Deubiquitinating Enzymes

ChemMedChem ◽  
2010 ◽  
Vol 5 (4) ◽  
pp. 552-558 ◽  
Author(s):  
Matteo Colombo ◽  
Stefania Vallese ◽  
Ilaria Peretto ◽  
Xavier Jacq ◽  
Jean-Christophe Rain ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Deubiquitinating Enzymes ◽  
Potential Inhibitors ◽  
Synthesis And Biological Evaluation

Synthesis and biological evaluation of new potential inhibitors of N-acylethanolamine hydrolyzing acid amidase

2010 ◽  
Vol 20 (3) ◽  
pp. 1210-1213 ◽  
Author(s):  
Carmela Saturnino ◽  
Stefania Petrosino ◽  
Alessia Ligresti ◽  
Chiara Palladino ◽  
Giovanni De Martino ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Potential Inhibitors ◽  
Synthesis And Biological Evaluation

Synthesis and biological evaluation of 3-benzyl-1-methyl- and 1-methyl-3-phenyl-isothioureas as potential inhibitors of iNOS

2005 ◽  
Vol 15 (3) ◽  
pp. 539-543 ◽  
Author(s):  
Nicola Paesano ◽  
Stefania Marzocco ◽  
Caterina Vicidomini ◽  
Carmela Saturnino ◽  
Giuseppina Autore ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Potential Inhibitors ◽  
Synthesis And Biological Evaluation

scholarly journals Synthesis and Biological Evaluation of Novel Jatrorrhizine Derivatives with Amino Groups Linked at the 3-Position as Inhibitors of Acetylcholinesterase

2017 ◽  
Vol 2017 ◽  
pp. 1-6 ◽  
Author(s):  
Xiaofei Jiang ◽  
Nengling Zhang ◽  
Nanqian Xiong ◽  
Yi Liu ◽  
Jianfeng Cao ◽  
...  
Keyword(s):  
Potent Inhibitor ◽  
Biological Evaluation ◽  
Lead Compound ◽  
Amino Groups ◽  
Coptis Chinensis ◽  
Inhibitor Activity ◽  
Active Constituents ◽  
Potential Inhibitors ◽  
Synthesis And Biological Evaluation

Jatrorrhizine was considered as one of the active constituents of Coptis chinensis Franch. Herein, jatrorrhizine derivatives with substituted amino groups linked at the 3-position were designed, synthesized, and biologically evaluated as inhibitors of acetylcholinesterase. Jatrorrhizine derivatives inhibited the activity of acetylcholinesterase (AChE) to a greater extent than the lead compound jatrorrhizine. All these jatrorrhizine derivatives were proved to be potent inhibitors of acetylcholinesterase (AChE) with submicromolar IC50 values, but less sensitive to butyrylcholinesterase (BuChE), which suggests that these jatrorrhizine derivatives are selective for AChE/BuChE. Compound 3g gave the most potent inhibitor activity for AChE (IC50 = 0.301 μM), which is greater than the lead compound jatrorrhizine. All these results demonstrated that these jatrorrhizine derivatives are potential inhibitors for AChE.

scholarly journals C-5 Aryl Substituted Azaspirooxindolinones Derivatives: Synthesis and Biological Evaluation as Potential Inhibitors of Tec Family Kinases

2021 ◽  
Author(s):  
Gopal Mudasani ◽  
Kalyani Paidikondala ◽  
Soňa Gurská ◽  
Shambabu Joseph Maddirala ◽  
Petr Džubák ◽  
...  
Keyword(s):  
Cell Lines ◽  
Biological Activities ◽  
Interleukin 2 ◽  
Biological Evaluation ◽  
Hematopoietic Malignancies ◽  
Bruton Tyrosine Kinase ◽  
Cyclopropyl Group ◽  
Tec Family Kinase ◽  
Potential Inhibitors ◽  
Synthesis And Biological Evaluation

<p>The interleukin-2-inducible kinase (ITK) and Bruton tyrosine kinase (BTK) are two crucial Tec family kinase members with important roles in the development of hematopoietic malignancies, autoimmune disorders and other diseases in human. Thus, ITK and BTK are key targets for drug development. Spirooxindoles are important scaffolds for the synthesis of small molecules with broad and potent biological activities. In this study, we performed a structure-activity relationship study of a new series of 5'-(benzo[d][1,3]dioxol-5-yl)spiro[piperidine-4,3'-pyrrolo[2,3-b]pyridin]-2'(1'H)-one linked with N-acyl and C-5 aryl-substituted scaffolds in a panel of ITK and BTK cancer cell lines. Four compounds <b>11</b>, <b>12</b>, <b>14</b> and <b>15</b> showed high antiproliferative activity against ITK and BTK cell lines. Compounds <b>11</b> and <b>12</b> with a C-5 benzodioxole group and gem-dialkyl group attached to carbonyl on piperidine were highly effective in ITK-high Jurkat and CEM cell lines, and compound <b>14, </b>a<strong> </strong>biotin analogue, was identified as a good inhibitor of BTK-high RAMOS cells. Compound <b>15 </b>with cyclopropyl group attached to carbonyl on piperidine also showed good activity in ITK and BTK cell lines.<b> </b></p>

Sign in / Sign up

Export Citation Format

Share Document