Relationships between DNA-binding kinetics and biological activity for the 9-aminoacridine-4-carboxamide class of antitumor agents

1987 ◽  
Vol 30 (5) ◽  
pp. 855-861 ◽  
Author(s):  
Laurence P. G. Wakelin ◽  
Graham J. Atwell ◽  
Gordon W. Rewcastle ◽  
William A. Denny
Keyword(s):  
Biological Activity ◽  
Dna Binding ◽  
Antitumor Agents ◽  
Binding Kinetics

Potential antitumor agents. 45. Synthesis, DNA-binding interaction, and biological activity of triacridine derivatives

1986 ◽  
Vol 29 (1) ◽  
pp. 69-74 ◽  
Author(s):  
Graham J. Atwell ◽  
Bruce C. Baguley ◽  
Dorota Wilmanska ◽  
William A. Denny
Keyword(s):  
Biological Activity ◽  
Dna Binding ◽  
Antitumor Agents ◽  
Binding Interaction ◽  
Potential Antitumor

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

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).

Isolation, Characterization, and DNA Binding Kinetics of Three Dirhodium(II,II) Carboxyamidate Complexes: Rh2(μ-L)(HNOCCF3)3where L= [OOCCH3]−, [OOCCF3]−, or [HNOCCF3]−

2011 ◽  
Vol 50 (8) ◽  
pp. 3458-3463 ◽  
Author(s):  
Shari U. Dunham ◽  
Todd S. Remaley ◽  
Bryn S. Moore ◽  
Debra L. Evans ◽  
Stephen U. Dunham
Keyword(s):  
Dna Binding ◽  
Binding Kinetics ◽  
Kinetics Of

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
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