scholarly journals SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF ESTER DERIVATIVES OF 4-(DIETHYLAMINO)SALICYLALDEHYDE AS CHOLINESTERASE, AND TYROSINASE INHIBITORS

2021 ◽  
Vol 7 (2) ◽  
pp. 137-144
Author(s):  
Reşit ÇAKMAK ◽  
Ercan ÇINAR ◽  
Eyüp BAŞARAN ◽  
Mehmet BOĞA
Keyword(s):  
Biological Evaluation ◽  
Tyrosinase Inhibitors ◽  
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.

Design and synthesis of herboxidiene derivatives that potently inhibit in vitro splicing

2021 ◽  
Vol 19 (6) ◽  
pp. 1365-1377
Author(s):  
Arun K. Ghosh ◽  
Srinivasa Rao Allu ◽  
Guddeti Chandrashekar Reddy ◽  
Adriana Gamboa Lopez ◽  
Patricia Mendez ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design And Synthesis ◽  
In Vitro Splicing ◽  
Enantioselective Syntheses ◽  
Derivatives Of

Enantioselective syntheses of C-6 modified derivatives of herboxidiene and their biological evaluation in splicing inhibitory assay.

scholarly journals Synthesis, characterization and biological activity of organometallic derivatives of the antimalarial drug mefloquine as new antischistosomal drug candidates

MedChemComm ◽  
2018 ◽  
Vol 9 (11) ◽  
pp. 1905-1909 ◽  
Author(s):  
Faustine d'Orchymont ◽  
Jeannine Hess ◽  
Gordana Panic ◽  
Marta Jakubaszek ◽  
Lea Gemperle ◽  
...  
Keyword(s):  
Biological Activity ◽  
Antimalarial Drug ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Drug Candidates ◽  
Derivatives Of

The design, synthesis, characterization and biological evaluation of new ferrocenyl and ruthenocenyl derivatives of the antimalarial mefloquine is described.

Solvent-free synthesis of novel vanillidene derivatives of Meldrum's acid: biological evaluation, DNA and BSA binding study

RSC Advances ◽  
2016 ◽  
Vol 6 (45) ◽  
pp. 39452-39459 ◽  
Author(s):  
Nenad Janković ◽  
Jovana Muškinja ◽  
Zoran Ratković ◽  
Zorica Bugarčić ◽  
Branislav Ranković ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Solvent Free ◽  
Binding Study ◽  
Meldrum's Acid ◽  
Meldrum’S Acid ◽  
Bsa Binding ◽  
Solvent Free Conditions ◽  
Derivatives Of ◽  
Solvent Free Synthesis

A series of novel O-alkyl vanillidene derivatives containing Meldrum's acid scaffold under solvent-free conditions were synthesized.

Synthesis and biological evaluation of novel 4-hydroxybenzaldehyde derivatives as tyrosinase inhibitors

2010 ◽  
Vol 45 (2) ◽  
pp. 639-646 ◽  
Author(s):  
Wei Yi ◽  
Rihui Cao ◽  
Wenlie Peng ◽  
Huan Wen ◽  
Qin Yan ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Tyrosinase Inhibitors ◽  
Synthesis And Biological Evaluation

ChemInform Abstract: Synthesis and Preliminary Biological Evaluation of New Derivatives of the Marine Alkaloid Leucettamine B as Kinase Inhibitors.

ChemInform ◽  
2010 ◽  
Vol 41 (23) ◽  
pp. no-no
Author(s):  
Mansour Debdab ◽  
Steven Renault ◽  
Olivier Lozach ◽  
Laurent Meijer ◽  
Ludovic Paquin ◽  
...  
Keyword(s):  
Kinase Inhibitors ◽  
Biological Evaluation ◽  
Marine Alkaloid ◽  
Derivatives Of
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