Synthesis and biological activity of selenopsammaplin A and its analogues as antitumor agents with DOT1L inhibitory activity

2021 ◽  
Vol 35 ◽  
pp. 116072 ◽  
Author(s):  
Hae Ju Han ◽  
Woong Sub Byun ◽  
Gyu Ho Lee ◽  
Won Kyung Kim ◽  
Kyungkuk Jang ◽  
...  
Keyword(s):  
Biological Activity ◽  
Inhibitory Activity ◽  
Antitumor Agents

1,3,4-Oxadiazole derivatives as potential antitumor agents: discovery, optimization and biological activity valuation

MedChemComm ◽  
2016 ◽  
Vol 7 (2) ◽  
pp. 263-271 ◽  
Author(s):  
Yin Luo ◽  
Zhi-Jun Liu ◽  
Guo Chen ◽  
Jing Shi ◽  
Jing-Ran Li ◽  
...  
Keyword(s):  
Biological Activity ◽  
Anticancer Activity ◽  
Active Compound ◽  
Inhibitory Activity ◽  
Antitumor Agents ◽  
Docking Simulation ◽  
Binding Model ◽  
Oxadiazole Derivatives ◽  
Potential Antitumor

New 1,3,4-oxadiazole derivatives have been synthesized and evaluated for their FAK inhibitory activity and anticancer activity. The most active compound 5h was studied by docking simulation to explore the binding model.

scholarly journals Synthesis of Novel Tryptamine Derivatives and Their Biological Activity as Antitumor Agents

Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 683
Author(s):  
Giorgia Simonetti ◽  
Carla Boga ◽  
Joseph Durante ◽  
Gabriele Micheletti ◽  
Dario Telese ◽  
...  
Keyword(s):  
Biological Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Solid Tumor ◽  
Antitumor Agents ◽  
Cancer Cell Lines ◽  
Hematological Cancer ◽  
Selective Effect ◽  
Ht29 Cells ◽  
High Level

We synthesized five novel tryptamine derivatives characterized by the presence of an azelayl chain or of a 1,1,1-trichloroethyl group, in turn connected to another heterocyclic scaffold. The combination of tryptamin-, 1,1,1-trichloroethyl- and 2-aminopyrimidinyl- moieties produced compound 9 identified as the most active compound in hematological cancer cell lines (IC50 = 0.57–65.32 μM). Moreover, keeping constant the presence of the tryptaminic scaffold and binding it to the azelayl moiety, the compounds maintain biological activity. Compound 13 is still active against hematological cancer cell lines and shows a selective effect only on HT29 cells (IC50 = 0.006 µM) among solid tumor models. Compound 14 loses activity on all leukemic lines, while showing a high level of toxicity on all solid tumor lines tested (IC50 0.0015–0.469 µM).

1-Methyl-3H-pyrazolo[1,2-a]benzo[1,2,3,4]tetrazin-3-ones. Design, Synthesis, and Biological Activity of New Antitumor Agents

2005 ◽  
Vol 48 (8) ◽  
pp. 2859-2866 ◽  
Author(s):  
Anna Maria Almerico ◽  
Francesco Mingoia ◽  
Patrizia Diana ◽  
Paola Barraja ◽  
Antonino Lauria ◽  
...  
Keyword(s):  
Biological Activity ◽  
Antitumor Agents ◽  
Design Synthesis

scholarly journals Design, Synthesis, and Biological Activity of Sulfonamide Analogues of Antofine and Cryptopleurine as Potent and Orally Active Antitumor Agents

2015 ◽  
Vol 58 (19) ◽  
pp. 7749-7762 ◽  
Author(s):  
Yongseok Kwon ◽  
Jayoung Song ◽  
Honggu Lee ◽  
Eun-Yeong Kim ◽  
Kiho Lee ◽  
...  
Keyword(s):  
Biological Activity ◽  
Antitumor Agents ◽  
Design Synthesis ◽  
Orally Active

Synthesis and biological activity of stable and potent antitumor agents, aniline nitrogen mustards linked to 9-anilinoacridines via a urea linkage

2008 ◽  
Vol 16 (10) ◽  
pp. 5413-5423 ◽  
Author(s):  
Naval Kapuriya ◽  
Kalpana Kapuriya ◽  
Xiuguo Zhang ◽  
Ting-Chao Chou ◽  
Rajesh Kakadiya ◽  
...  
Keyword(s):  
Biological Activity ◽  
Antitumor Agents ◽  
Nitrogen Mustards

Exploring QSAR on 3-aminopyrazoles as antitumor agents for their inhibitory activity of CDK2/cyclin A

2006 ◽  
Vol 41 (10) ◽  
pp. 1190-1195 ◽  
Author(s):  
Soma Samanta ◽  
Bikash Debnath ◽  
Anindya Basu ◽  
Shovanlal Gayen ◽  
Kolluru Srikanth ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Antitumor Agents ◽  
Cyclin A

scholarly journals Isolation and Cholinesterase Inhibitory Activity of Narcissus Extracts and Amaryllidaceae Alkaloid

2013 ◽  
Vol 8 (6) ◽  
pp. 1934578X1300800 ◽  
Author(s):  
Lucie Cahlíková ◽  
Miroslav Ločárek ◽  
Nina Benešová ◽  
Radim Kučera ◽  
Jakub Chlebek ◽  
...  
Keyword(s):  
Biological Activity ◽  
Inhibitory Activity ◽  
Mass Spectra ◽  
Dependent Manner ◽  
Inhibition Activity ◽  
Narcissus Poeticus ◽  
Cholinesterase Inhibitory Activity ◽  
Alkaloid Extracts ◽  
Dose Dependent ◽  
Retention Indexes

Alkaloid extracts of eleven Narcissus (Amaryllidaceae) species and varieties were studied with respect to their acetylcholinesterase (HuAChE) and butyrylcholinesterase (HuBuChE) inhibitory activity and alkaloid patterns. Forty-two alkaloids were determined by GC/MS, and thirty of them identified from their mass spectra, retention times and retention indexes. Promising HuAChE inhibition activity was demonstrated by nine Narcissus taxa and HuBuChE inhibition by Narcissus poeticus cv. Pink Parasol with an IC50 value of 3.3 ± 0.5 μg/mL. The alkaloid identified as (11C- S)-homolycorine was isolated in pure form from Narcissus Sir W. Churchill using preparative TLC and was tested for its biological activity. Homolycorine inhibited HuAChE and HuBuChE in a dose-dependent manner with IC50 values of 63.7±4.3 μM and 151.0±15.2 μM, respectively.

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