Antitumor activity studies of iridium (III) polypyridine complexes-loaded liposomes against gastric tumor cell in vitro

Murine leukemic cells, after in vivo treatment with antineoplastic drugs, have been shown to express new antigenic specificities that were not detectable on parental cells and that were heritable after the withdrawal of drug treatment. A study was conducted of macrophage antitumor activity triggered by LY/DTIC cells, a subline of LY murine lymphoma, antigenically altered by the drug DTIC. In vitro non-specific inhibition of tumor cell growth was exhibited by spleen and peritoneal macrophages from mice previously challenged with viable LY/DTIC. Peritoneal macrophages from LY/DTIC immune animals showed moderate, although significant lytic activity against unrelated tumor target cells. Supernatants from mixed lymphocyte-tumor cell cultures, in which LY/DTIC immune lymphocytes and LY/DTIC tumor cells had been cultured, rendered normal macrophages non-specifically growth inhibitory for tumor cells.

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Antitumor Activity In Vitro Provided by N-Alkyl-Nitroimidazole Compounds

The Open Medicinal Chemistry Journal ◽

10.2174/1874104502014010045 ◽

2020 ◽

Vol 14 (1) ◽

pp. 45-48

Author(s):

Janny A. Villa-Pulgarin ◽

Constain H. Salamanca ◽

Jose Oñate-Garzón ◽

Ruben E Varela-M

Keyword(s):

Antitumor Activity ◽

Tumor Cell ◽

Cell Lines ◽

Alkyl Chain ◽

Imidazole Ring ◽

Antitumoral Activity ◽

Lung Cells ◽

Tumor Cell Lines ◽

A549 Lung

Background: Cancer is one of the most common diseases in the world, with over 18 million new cases estimated in 2018. Many of the drugs used for cancer can have significant adverse effects and variable effectiveness. Nitroimidazoles are prodrugs that usually have shown antimicrobial activity specifically antiparasitic. However, its antitumor activity in vitro has barely been explored. Objective: The aim of this study is to determine the influence of the length of the substituted N-alkyl chain in the imidazole ring on the antitumor activity in vitro. Methods: Four nitroimidazoles were obtained by chemical synthesis varying the length of the substituted N-alkyl chain from methyl to butyl. The antitumor activity of N-alkyl-nitroimidazoles was evaluated by MTT assay employing two tumor cell lines (MDA-MB231 and A549). Results: In this study, it was reported that N-alkyl nitroimidazoles exhibited an LC50 as low as 16.7 µM in breast tumor cells MDA-MB231 while in normal Vero kidney cells, the LC50 was around 30 µM. It was also reported that the length of the substituted N-Alkyl chain in the imidazole ring affects the antitumoral activity in A549 lung cells. Conclusion: Increasing the length of the substituted N-Alkyl chain in the imidazole ring decreased the antitumor activity against only A549 cancer cells. N-alkyl nitroimidazoles exhibited considerable selectivity towards tumor cell lines.

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Bimetallic Catalyzed N-arylation Used in Synthesis of Novel β-carbolines Derivatives

Letters in Drug Design & Discovery ◽

10.2174/1570180815666181025124615 ◽

2020 ◽

Vol 17 (5) ◽

pp. 520-525

Author(s):

Rui Cai ◽

Li Zhu ◽

Pengfei Wang ◽

Yu Zhao

Keyword(s):

Antitumor Activity ◽

Tumor Cell ◽

13C Nmr ◽

Antiproliferative Activity ◽

Pyridine Ring ◽

Catalyst System ◽

Tumor Cell Lines ◽

Antitumor Activities ◽

Acid Condition

Background: Natural occurring β-Carbolines alkaloids are abundant in the plant kingdom or other organisms, and they were found to possess good antitumor activity through multiple mechanisms. Based on previous summarized SARs of β-carboline derivatives, the modification on pyridine ring would have a great impact on their antitumor activities. Therefore, we plan to synthesized arylated β-carboline-3-amides to find more valuable β-Carbolines derivatives. Methods: A novel bimetallic Pd(OAc)2/AgOAc catalyst system was developed for the amidation of aryl iodides under acid condition. A series of N-arylated β-carbolines derivatives were synthesized using this method. The structures of these compounds were confirmed by 1H NMR, 13C NMR and HRMS, and their in vitro antiproliferative activity was investigated against HepG2 and Hela tumor cell lines by MTT assay. Results: Eleven N-arylated β-carboline-3-amides were synthesized using this bimetallic catalyzed method in 58-98% yields. These synthesized N-arylated compounds showed no antiproliferative activity at 20 μM. Conclusion: We have discovered an efficient and bimetallic catalytic system allowing the Narylation of secondary acyclic amides. This is the first report that N-arylation of aliphatic secondary acyclic amides under acid condition.

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Antiproliferative and Antitumor Activity of the 2-Cyanoaziridine Compound Imexon on Tumor Cell Lines and Fresh Tumor Cells In Vitro

JNCI Journal of the National Cancer Institute ◽

10.1093/jnci/84.16.1238 ◽

1992 ◽

Vol 84 (16) ◽

pp. 1238-1244 ◽

Cited By ~ 20

Author(s):

E. M. Hersh ◽

C. R. Gschwind ◽

C. W. Taylor ◽

R. T. Dorr ◽

R. Taetle ◽

...

Keyword(s):

Antitumor Activity ◽

Tumor Cell ◽

Tumor Cells ◽

Cell Lines ◽

Tumor Cell Lines

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Synthesis and biological activity of (S)-2′-fluorodaunorubicin

Canadian Journal of Chemistry ◽

10.1139/v88-030 ◽

1988 ◽

Vol 66 (1) ◽

pp. 187-190 ◽

Cited By ~ 18

Author(s):

Hans H. Baer ◽

Lisa Siemsen

Keyword(s):

Biological Activity ◽

Antitumor Activity ◽

Tumor Cell ◽

Cell Lines ◽

Title Compound ◽

Free Sugar ◽

Tumor Cell Lines ◽

Murine Leukemia

Methyl 3-amino-2,3,6-trideoxy-2-fluoro-β-L-galactopyranoside was hydrolyzed to the free sugar, (S)-2-fluorodaunosamine hydrochloride, which was converted into the α,β-1,4-di-O-acetyl-N-trifluoroacetyl derivative and thence into the corresponding glycosyl bromide. The latter was condensed with daunomycinone, and the product was deprotected to give the title compound. The fluoroanthracycline displayed significant cytotoxicity against a number of tumor cell lines in vitro. Antitumor activity against L1210 murine leukemia in vivo was lower than that of the parent daunorubicin, but toxicity appeared to be reduced.

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Antitumor activity of tricyclic pyrone analogs, a new synthetic class of microtubule de-stabilizing agents, in the murine EMT-6 mammary tumor cell line in vitro

Anti-Cancer Drugs ◽

10.1097/00001813-199807000-00008 ◽

1998 ◽

Vol 9 (6) ◽

pp. 565-576 ◽

Cited By ~ 8

Author(s):

Elisabeth M Perchellet ◽

James B Ladesich ◽

Yi Chen ◽

Hong-Sig Sin ◽

Duy H Hua ◽

...

Keyword(s):

Antitumor Activity ◽

Tumor Cell ◽

Cell Line ◽

Mammary Tumor ◽

Tumor Cell Line ◽

Mammary Tumor Cell ◽

Mammary Tumor Cell Line ◽

Stabilizing Agents

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Synthesis and Antitumor Activity Assay of Epoxy Bicyclo[4.2.2]deca-2,4,7,(9)- tri(tetra)enes and Tricyclo[9.4.2.02,10]heptadeca-2,12,14,16-tetraene

Current Organic Chemistry ◽

10.2174/1385272823666190621104843 ◽

2019 ◽

Vol 23 (10) ◽

pp. 1158-1165

Author(s):

Vladimir A. D'yakonov ◽

Gulnara N. Kadikova ◽

Guzel F. Gazizullina ◽

Lilya U. Dzhemileva ◽

Artur R. Tulyabaev ◽

...

Keyword(s):

Antitumor Activity ◽

Tumor Cell ◽

Tumor Cell Lines ◽

Activity Assay ◽

X Ray Diffraction ◽

X Ray ◽

High Antitumor Activity ◽

High Yields ◽

First Time

Triepoxides were synthesized for the first time in high yields (80-85%) by oxidation of substituted bicyclo[4.2.2]deca-2,4,7,9-tetraenes, bicyclo[4.2.2]deca-2,4,7-trienes, and tricyclo[9.4.2.02,10]heptadeca-2,12,14,16-tetraene with an excess of m-chloroperbenzoic acid. The structures of the epoxy derivatives were reliably proved using modern spectral methods and X-ray diffraction analysis. A high antitumor activity in vitro was found for triepoxides against the Jurkat, K562, U937 tumor cell lines and normal fibroblasts.

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