N-phosphinyl ureas: Synthesis, characterization, X-ray structure, and in vitro evaluation of antitumor activity

A series of bimetallic dppfM(II) (dppf = 1,1’-bis (diphenyphosphino) ferrocene; M = Pt and Pd) dithiocarbamate complexes is synthesized and characterized by spectroscopic methods and single-crystal X-ray diffraction. Their antitumor activities in vitro are investigated by MTT assays against four cancer cell lines. The anticancer studies indicate most of the complexes display good to excellent antitumor activity. Remarkably, the platinum complex with a pyrrolidinyl substituent (3b) was identified as the most promising candidate due to its high potency and broad spectrum of activity.

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Synthesis, X-ray Diffraction Structures, Spectroscopic Properties, and in vitro Antitumor Activity of Isomeric (1H-1,2,4-Triazole)Ru(III) Complexes

Inorganic Chemistry ◽

10.1021/ic034605i ◽

2003 ◽

Vol 42 (19) ◽

pp. 6024-6031 ◽

Cited By ~ 67

Author(s):

Vladimir B. Arion ◽

Erwin Reisner ◽

Madeleine Fremuth ◽

Michael A. Jakupec ◽

Bernhard K. Keppler ◽

...

Keyword(s):

Antitumor Activity ◽

Spectroscopic Properties ◽

X Ray Diffraction ◽

X Ray

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Preparation of bis(5-phenyltetrazolato) Pt(II) and Pt(IV) analogues of transplatin and in vitro evaluation for antitumor activity

Inorganica Chimica Acta ◽

10.1016/j.ica.2016.11.017 ◽

2017 ◽

Vol 456 ◽

pp. 86-94 ◽

Cited By ~ 3

Author(s):

Stefanie Perfahl ◽

Anja Bodtke ◽

Jitka Pracharova ◽

Jana Kasparkova ◽

Viktor Brabec ◽

...

Keyword(s):

Antitumor Activity ◽

In Vitro Evaluation

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In vitro evaluation of antitumor activity of doxorubicin-loaded nanoemulsion in MCF-7 human breast cancer cells

Journal of Nanoparticle Research ◽

10.1007/s11051-013-1489-5 ◽

2013 ◽

Vol 15 (3) ◽

Cited By ~ 4

Author(s):

Mayson H. Alkhatib ◽

Hayat M. AlBishi

Keyword(s):

Breast Cancer ◽

Antitumor Activity ◽

Cancer Cells ◽

Human Breast Cancer ◽

Breast Cancer Cells ◽

Human Breast Cancer Cells ◽

Human Breast ◽

In Vitro Evaluation ◽

Mcf 7

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Comparison of two kinds of docetaxel-vitamin E prodrugs: In vitro evaluation and in vivo antitumor activity

International Journal of Pharmaceutics ◽

10.1016/j.ijpharm.2016.03.057 ◽

2016 ◽

Vol 505 (1-2) ◽

pp. 352-360 ◽

Cited By ~ 2

Author(s):

Jing Wang ◽

Peng Xue ◽

Jiahua Zhou ◽

Lin Li ◽

Lu Xu ◽

...

Keyword(s):

Vitamin E ◽

Antitumor Activity ◽

In Vitro Evaluation ◽

In Vivo Antitumor Activity

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Synthesis, Characterization and In Vitro Evaluation of Novel 5-Ene-thiazolo[3,2-b][1,2,4]triazole-6(5H)-ones as Possible Anticancer Agents

Molecules ◽

10.3390/molecules26041162 ◽

2021 ◽

Vol 26 (4) ◽

pp. 1162

Author(s):

Serhii Holota ◽

Sergiy Komykhov ◽

Stepan Sysak ◽

Andrzej Gzella ◽

Andriy Cherkas ◽

...

Keyword(s):

Antitumor Activity ◽

Cell Lines ◽

Cancer Cell ◽

Anticancer Agents ◽

Cancer Cell Lines ◽

Hek293 Cells ◽

In Vitro Evaluation ◽

Anticancer Properties ◽

Sar Study

The present paper is devoted to the search for drug-like molecules with anticancer properties using the thiazolo[3,2-b][1,2,4]triazole-6-one scaffold. A series of 24 novel thiazolo-[3,2-b][1,2,4]triazole-6-ones with 5-aryl(heteryl)idene- and 5-aminomethylidene-moieties has been synthesized employing three-component and three-stage synthetic protocols. A mixture of Z/E-isomers was obtained in solution for the synthesized 5-aminomethylidene-thiazolo[3,2-b]-[1,2,4]triazole-6-ones. The compounds have been studied for their antitumor activity in the NCI 60 lines screen. Some compounds present excellent anticancer properties at 10 μM. Derivatives 2h and 2i were the most active against cancer cell lines without causing toxicity to normal somatic (HEK293) cells. A preliminary SAR study had been performed for the synthesized compounds.

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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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