ChemInform Abstract: Effect of Modification of 6-[(Aminoalkyl)amino]-7H-benzo[e]perimidin-7-ones on Their Cytotoxic Activity Toward Sensitive and Multidrug Resistant Tumor Cell Lines. Synthesis and Biological Evaluation.

ChemInform ◽  
2010 ◽  
Vol 33 (20) ◽  
pp. no-no
Author(s):  
Maria Dzieduszycka ◽  
Sante Martelli ◽  
Malgorzata Arciemiuk ◽  
Maria M. Bontemps-Gracz ◽  
Agnieszka Kupiec ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Multidrug Resistant ◽  
Biological Evaluation ◽  
Tumor Cell Lines ◽  
Synthesis And Biological Evaluation

Synthesis and biological evaluation of novel derivatives of gambogenic acid as anticancer agents

MedChemComm ◽  
2015 ◽  
Vol 6 (2) ◽  
pp. 334-338 ◽  
Author(s):  
Peng Huang ◽  
Zhong Hu ◽  
Liqin He ◽  
Xiaoshan Wang ◽  
Yaxian Wu
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Antiproliferative Activity ◽  
Biological Evaluation ◽  
Tumor Cell Lines ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

A series of novel derivatives of gambogenic acid (GNA) were synthesized and evaluated for their in vitro antiproliferative activity against four kinds of tumor cell lines. These compounds displayed potent antiproliferative activity. In particular, compound 3f exhibited superior antiproliferative activity against these tumor cell lines than GNA.

Differential Increases in Glutathione S-Transferase Activities in a Range of Multidrug-Resistant Human Tumor Cell Lines

1989 ◽  
Vol 1 (6) ◽  
pp. 359-365 ◽  
Author(s):  
Richard D. H. Whelan ◽  
Louise K. Hosking ◽  
Alan J. Townsend ◽  
Kenneth H. Cowan ◽  
Bridget T. Hill
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Human Tumor ◽  
Multidrug Resistant ◽  
Tumor Cell Lines ◽  
Glutathione S Transferase ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines

Synthesis and Biological Evaluation of Novel 4,5,6,7-Tetrahydrobenzo[D]-Thiazol-2- Yl Derivatives Derived from Dimedone with Anti-Tumor, C-Met, Tyrosine Kinase and Pim-1 Inhibitions

2019 ◽  
Vol 19 (12) ◽  
pp. 1438-1453 ◽  
Author(s):  
Rafat M. Mohareb ◽  
Amr S. Abouzied ◽  
Nermeen S. Abbas
Keyword(s):  
Tyrosine Kinase ◽  
Tumor Cell ◽  
Cell Lines ◽  
Single Molecule ◽  
Anticancer Agents ◽  
Biological Evaluation ◽  
New Drugs ◽  
Tumor Cell Lines ◽  
Thiazole Derivatives ◽  
Wide Range

Background: Dimedone and thiazole moieties are privileged scaffolds (acting as primary pharmacophores) in many compounds that are useful to treat several diseases, mainly tropical infectious diseases. Thiazole derivatives are a very important class of compounds due to their wide range of pharmaceutical and therapeutic activities. On the other hand, dimedone is used to synthesize many therapeutically active compounds. Therefore, the combination of both moieties through a single molecule to produce heterocyclic compounds will produce excellent anticancer agents. Objective: The present work reports the synthesis of 47 new substances belonging to two classes of compounds: Dimedone and thiazoles, with the purpose of developing new drugs that present high specificity for tumor cells and low toxicity to the organism. To achieve this goal, our strategy was to synthesize a series of 4,5,6,7-tetrahydrobenzo[d]-thiazol-2-yl derivatives using the reaction of the 2-bromodimedone with cyanothioacetamide. Methods: The reaction of 2-bromodimedone with cyanothioacetamide gave the 4,5,6,7-tetrahydrobenzo[d]- thiazol-2-yl derivative 4. The reactivity of compound 4 towards some chemical reagents was observed to produce different heterocyclic derivatives. Results: A cytotoxic screening was performed to evaluate the performance of the new derivatives in six tumor cell lines. Thirteen compounds were shown to be promising toward the tumor cell lines which were further evaluated toward five tyrosine kinases. Conclusion: The results of antitumor screening showed that many of the tested compounds were of high inhibition towards the tested cell lines. Compounds 6c, 8c, 11b, 11d, 13b, 14b, 15c, 15g, 21b, 21c, 20d and 21d were the most potent compounds toward c-Met kinase and PC-3 cell line. The most promising compounds 6c, 8c, 11b, 11d, 13b, 14b, 15c, 15g, 20c, 20d, 21b, 21c and 21d were further investigated against tyrosine kinase (c-Kit, Flt-3, VEGFR-2, EGFR, and PDGFR). Compounds 6c, 11b, 11d, 14b, 15c, and 20d were selected to examine their Pim-1 kinase inhibition activity the results revealed that compounds 11b, 11d and 15c had high activities.

C-prenylated flavonoids with potential cytotoxic activity against solid tumor cell lines

2019 ◽  
Vol 18 (4) ◽  
pp. 1051-1100
Author(s):  
Lenka Molčanová ◽  
Dominika Janošíková ◽  
Stefano Dall´Acqua ◽  
Karel Šmejkal
Keyword(s):  
Tumor Cell ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Solid Tumor ◽  
Tumor Cell Lines ◽  
Prenylated Flavonoids

Molecular modeling of cytotoxic activity of a new terpenoid-like bischalcone

2019 ◽  
Vol 43 (47) ◽  
pp. 18451-18460
Author(s):  
Lóide O. Sallum ◽  
Vera L. Siqueira ◽  
Jean M. F. Custodio ◽  
Nádia M. Borges ◽  
Aliny P. Lima ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Molecular Modeling ◽  
Tumor Cell ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Tumor Cell Lines

This study describes the synthesis and structure of (1E,4E)-1-(3-chlorophenyl)-5-(2,6,6-trimethylcyclohex-1-en-1-yl)penta-1,4-dien-3-one (BC I). This work evaluates molecular docking and cytotoxic activity against two tumor cell lines.

scholarly journals Selective cytotoxic activity of brefeldin A against human tumor cell lines.

1989 ◽  
Vol 42 (12) ◽  
pp. 1877-1878 ◽  
Author(s):  
SHIGETAKA ISHII ◽  
MIEKO NAGASAWA ◽  
YUKO KARIYA ◽  
HARUO YAMAMOTO
Keyword(s):  
Tumor Cell ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Human Tumor ◽  
Brefeldin A ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines
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