Synthesis, characterisation and in vitro cytotoxicity of mixed ligand Pt(ii) oxadiazoline complexes with hexamethylenetetramine and 7-nitro-1,3,5-triazaadamantane

2017 ◽  
Vol 46 (36) ◽  
pp. 12226-12238 ◽  
Author(s):  
Stefanie Sieste ◽  
Irina Lifincev ◽  
Nina Stein ◽  
Gabriele Wagner
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
In Vitro Cytotoxicity ◽  
Mixed Ligand ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines

The synthesis, spectroscopic and DFT-computational characterisation of trans-Pt(ii) oxadiazoline complexes is described. Some are more cytotoxic in vitro than cisplatin with the human cancer cell lines HeLa and A549.

scholarly journals In vitro cytotoxicity of Indonesian stingless bee products against human cancer cell lines

2014 ◽  
Vol 4 (7) ◽  
pp. 549-556 ◽  
Author(s):  
Paula M. Kustiawan ◽  
Songchan Puthong ◽  
Enos T. Arung ◽  
Chanpen Chanchao
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
In Vitro Cytotoxicity ◽  
Stingless Bee ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines

In vitro cytotoxicity against different human cancer cell lines of laticifer proteins of Calotropis procera (Ait.) R. Br

2007 ◽  
Vol 21 (8) ◽  
pp. 1563-1573 ◽  
Author(s):  
Jefferson Soares de Oliveira ◽  
Daniel Pereira Bezerra ◽  
Cleverson Diniz Teixeira de Freitas ◽  
José Delano Barreto Marinho Filho ◽  
Manoel Odorico de Moraes ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
In Vitro Cytotoxicity ◽  
Calotropis Procera ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines

Evaluation of in vitro cytotoxicity of one-dimensional chain [Fe(salen)(L)]n complexes against human cancer cell lines

2012 ◽  
Vol 26 (3) ◽  
pp. 480-484 ◽  
Author(s):  
Zdeněk Dvořák ◽  
Pavel Štarha ◽  
Zdeněk Šindelář ◽  
Zdeněk Trávníček
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
In Vitro Cytotoxicity ◽  
Dimensional Chain ◽  
Human Cancer Cell ◽  
One Dimensional ◽  
Human Cancer Cell Lines

scholarly journals Discovery of New Pyrazolopyridine, Furopyridine, and Pyridine Derivatives as CDK2 Inhibitors: Design, Synthesis, Docking Studies, and Anti-Proliferative Activity

Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 3923
Author(s):  
Adel A.-H. Abdel-Rahman ◽  
Amira K. F. Shaban ◽  
Ibrahim F. Nassar ◽  
Dina S. EL-Kady ◽  
Nasser S. M. Ismail ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Molecular Docking Study ◽  
Human Cancer Cell Lines ◽  
Hct 116 ◽  
Mcf 7

New pyridine, pyrazoloyridine, and furopyridine derivatives substituted with naphthyl and thienyl moieties were designed and synthesized starting from 6-(naphthalen-2-yl)-2-oxo-4-(thiophen-2-yl)-1,2-dihydropyridine-3-carbonitrile (1). The chloro, methoxy, cholroacetoxy, imidazolyl, azide, and arylamino derivatives were prepared to obtain the pyridine-−C2 functionalized derivatives. The derived pyrazolpyridine-N-glycosides were synthesized via heterocyclization of the C2-thioxopyridine derivative followed by glycosylation using glucose and galactose. The furopyridine derivative 14 and the tricyclic pyrido[3′,2′:4,5]furo[3,2-d]pyrimidine 15 were prepared via heterocyclization of the ester derivative followed by a reaction with formamide. The newly synthesized compounds were evaluated for their ability to in vitro inhibit the CDK2 enzyme. In addition, the cytotoxicity of the compounds was tested against four different human cancer cell lines (HCT-116, MCF-7, HepG2, and A549). The CDK2/cyclin A2 enzyme inhibitory results revealed that pyridone 1, 2-chloro-6-(naphthalen-2-yl)-4-(thiophen-2-yl)nicotinonitrile (4), 6-(naphthalen-2-yl)-4-(thiophen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-amine (8), S-(3-cyano-6-(naphthaen-2-yl)-4-(thiophen-2-yl)pyridin-2-yl) 2-chloroethanethioate (11), and ethyl 3-amino-6-(naphthalen-2-yl)-4-(thiophen-2-yl)furo[2,3-b]pyridine-2-carboxylate (14) are among the most active inhibitors with IC50 values of 0.57, 0.24, 0.65, 0.50, and 0.93 µM, respectively, compared to roscovitine (IC50 0.394 μM). Most compounds showed significant inhibition on different human cancer cell lines (HCT-116, MCF-7, HepG2, and A549) with IC50 ranges of 31.3–49.0, 19.3–55.5, 22.7–44.8, and 36.8–70.7 μM, respectively compared to doxorubicin (IC50 40.0, 64.8, 24.7 and 58.1 µM, respectively). Furthermore, a molecular docking study suggests that most of the target compounds have a similar binding mode as a reference compound in the active site of the CDK2 enzyme. The structural requirements controlling the CDK2 inhibitory activity were determined through the generation of a statistically significant 2D-QSAR model.

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