Synthesis, Biochemical, and Biological Evaluation of C2 Linkage Derivatives of Amino Sugars, Inhibitors of Glucokinase from Trypanosoma cruzi

2021 ◽  
pp. 128227
Author(s):  
Scott B. Gree ◽  
Robert J. Lanier Jr ◽  
Shane M. Carey ◽  
David R. Morgan ◽  
Hanna Gracz ◽  
...  
Keyword(s):  
Trypanosoma Cruzi ◽  
Biological Evaluation ◽  
Amino Sugars ◽  
Derivatives Of

Design, synthesis and biological evaluation of hybrid bioisoster derivatives of N-acylhydrazone and furoxan groups with potential and selective anti-Trypanosoma cruzi activity

2014 ◽  
Vol 82 ◽  
pp. 418-425 ◽  
Author(s):  
Ricardo Augusto Massarico Serafim ◽  
José Eduardo Gonçalves ◽  
Felipe Pereira de Souza ◽  
Ana Paula de Melo Loureiro ◽  
Silvia Storpirtis ◽  
...  
Keyword(s):  
Trypanosoma Cruzi ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

scholarly journals Pyrazol(in)e derivatives of curcumin analogs as a new class of anti-Trypanosoma cruzi agents

2021 ◽  
Author(s):  
Dimitris Matiadis ◽  
Tatiana Saporiti ◽  
Elena Aguilera ◽  
Xavier Robert ◽  
Christophe Guillon ◽  
...  
Keyword(s):  
Trypanosoma Cruzi ◽  
Mammalian Cells ◽  
Triosephosphate Isomerase ◽  
Biological Evaluation ◽  
Significant Activity ◽  
New Class ◽  
New Family ◽  
Curcumin Analogs ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

Aim: We report the synthesis and biological evaluation of a small library of 15 functionalized 3-styryl-2-pyrazolines and pyrazoles, derived from curcuminoids, as trypanosomicidal agents. Methods & results: The compounds were prepared via a cyclization reaction between the corresponding curcuminoids and the appropriate hydrazines. All of the derivatives synthesized were investigated for their trypanosomicidal activities. Compounds 4a and 4e showed significant activity against epimastigotes of Trypanosoma cruzi, with IC50 values of 5.0 and 4.2 μM, respectively, accompanied by no toxicity to noncancerous mammalian cells. Compound 6b was found to effectively inhibit T. cruzi triosephosphate isomerase. Conclusion: The up to 16-fold higher potency of these derivatives compared with their curcuminoid precursors makes them a promising new family of T. cruzi inhibitors.

Synthesis, molecular docking and biological evaluation of novel phthaloyl derivatives of 3-amino-3-aryl propionic acids as inhibitors of Trypanosoma cruzi trans-sialidase

2018 ◽  
Vol 156 ◽  
pp. 252-268 ◽  
Author(s):  
Muhammad Kashif ◽  
Karla Fabiola Chacón-Vargas ◽  
Julio Cesar López-Cedillo ◽  
Benjamín Nogueda-Torres ◽  
Alma D. Paz-González ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Trypanosoma Cruzi ◽  
Biological Evaluation ◽  
Derivatives Of

Synthesis, Structural Studies and Biological Evaluation of Halogen Derivatives of 1,3-Disubstituted Thiourea

2017 ◽  
Vol 14 (6) ◽  
Author(s):  
Anna Bielenica ◽  
Karolina Stepien ◽  
Aleksandra Sawczenko ◽  
Tadeusz Lis ◽  
Anna E. Koziol ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Structural Studies ◽  
Derivatives Of

Design, Synthesis and Biological Evaluation of Novel Aminosaccharide Derivatives of Combretastatin A-4

2013 ◽  
Vol 10 (10) ◽  
pp. 935-941
Author(s):  
Yan Tang ◽  
Zhewei Tu ◽  
Jing Sun ◽  
Xiong Zhu ◽  
Kun Liu ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

Hybridized Quinoline Derivatives as Anticancer Agents: Design, Synthesis, Biological Evaluation and Molecular Docking

2019 ◽  
Vol 19 (4) ◽  
pp. 439-452 ◽  
Author(s):  
Mohamed R. Selim ◽  
Medhat A. Zahran ◽  
Amany Belal ◽  
Moustafa S. Abusaif ◽  
Said A. Shedid ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Anticancer Agents ◽  
Caspase 3 ◽  
Biological Evaluation ◽  
Tubulin Polymerization ◽  
Design Synthesis ◽  
Chemical Structures ◽  
M Phase ◽  
Induced Apoptosis ◽  
Derivatives Of

Objective: Conjugating quinolones with different bioactive pharmacophores to obtain potent anticancer active agents. Methods: Fused pyrazolopyrimidoquinolines 3a-d, Schiff bases 5, 6a-e, two hybridized systems: pyrazolochromenquinoline 7 and pyrazolothiazolidinquinoline 8, different substituted thiazoloquinolines 13-15 and thiazolo[3,2-a]pyridine derivatives 16a-c were synthesized. Their chemical structures were characterized through spectral and elemental analysis, cytotoxic activity on five cancer cell lines, caspase-3 activation, tubulin polymerization inhibition and cell cycle analysis were evaluated. Results: Four compounds 3b, 3d, 8 and 13 showed potent activity than doxorubicin on HCT116 and three compounds 3b, 3d and 8 on HEPG2. These promising derivatives showed increase in the level of caspase-3. The trifloromethylphenyl derivatives of pyrazolopyrimidoquinolines 3b and 3d showed considerable tubulin polymerization inhibitory activity. Both compounds arrested cell cycle at G2/M phase and induced apoptosis. Conclusion: Compounds 3b and 3d can be considered as promising anticancer active agents with 70% of colchicine activity on tubulin polymerization inhibition and represent hopeful leads that deserve further investigation and optimization.

Amino sugars. XXVII. The synthesis of derivatives of 3-amino-3,4,6-trideoxy-D- or L-xylo-hexopyranose

1972 ◽  
Vol 37 (9) ◽  
pp. 2985-2993 ◽  
Author(s):  
K. Kefurt ◽  
K. Čapek ◽  
J. Čapková ◽  
Z. Kefurtová ◽  
J. Jarý
Keyword(s):  
Amino Sugars ◽  
Derivatives Of
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