scholarly journals Synthesis of chimeric amides of 2-arilaminopyrimidine series

2020 ◽  
Vol 56 (2) ◽  
pp. 166-180
Author(s):  
Zh. V. Ignatovich
Keyword(s):  
Antitumor Activity ◽  
Antitumor Drugs ◽  
Methodological Approaches ◽  
Amino Pyrimidine ◽  
Chimeric Molecules ◽  
Pyrimidine Fragment

Methodological approaches to the synthesis of 2-arylpyrimidine amides with predicted antitumor activity using the design of chimeric molecules by combining pharmacophore fragments of known antitumor drugs are considered. The results of the synthesis of chimeric amides containing, along with the 2-amino-pyrimidine fragment, fragments of other nitrogen and oxygen-containing heterocycles (piperazine, morpholine, isoxazole, etc.), aromatic cycles (benzene, methylnitroaniline, phenylenediamine) and functional (methyl-, amino-, carboxy-, etc.) groups in different positions of the molecule, are presented.

Evaluation of antitumor activities of hyaluronate binding antitumor drugs: synthesis, characterization and antitumor activity

1996 ◽  
Vol 4 (1) ◽  
pp. 1-8 ◽  
Author(s):  
Kazuo Akima ◽  
Hisashi Ito ◽  
Yuhei Iwata ◽  
Kayoko Matsuo ◽  
Nobutoshi Watari ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Antitumor Drugs ◽  
Antitumor Activities

In Vitro Antitumor Activity of 9-Nitro-Camptothecin as a Single Agent and in Combination with other Antitumor Drugs

2006 ◽  
Vol 922 (1) ◽  
pp. 293-297 ◽  
Author(s):  
RALPH J. BERNACKI ◽  
PAULA PERA ◽  
PETER GAMBACORTA ◽  
YSEULT BRUN ◽  
WILLIAM R. GRECO
Keyword(s):  
Antitumor Activity ◽  
Single Agent ◽  
Antitumor Drugs

Self-assembly of pH-responsive dextran-g-poly(lactide-co-glycolide)-g-histidine copolymer micelles for intracellular delivery of paclitaxel and its antitumor activity

RSC Advances ◽  
2016 ◽  
Vol 6 (28) ◽  
pp. 23693-23701 ◽  
Author(s):  
Jiulong Zhang ◽  
Kang Chen ◽  
Ying Ding ◽  
Xiu Xin ◽  
Wenpan Li ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Self Assembly ◽  
Intracellular Delivery ◽  
Antitumor Drugs ◽  
Ph Responsive ◽  
Copolymer Micelles

Herein, dextran (DX) was conjugated with poly(lactide-co-glycolide) (PLGA) and histidine (His) to prepare a pH-responsive nanocarrier, dextran-g-poly(lactide-co-glycolide)-g-histidine (HDP) micelles, for the delivery of antitumor drugs.

scholarly journals Indolo[2,3-a]carbazole Derivatives with Antitumor Activity and Instrumental Methods for Their Investigation (Review)

2020 ◽  
Vol 9 (4) ◽  
pp. 128-135
Author(s):  
D. A. Kozin ◽  
Z. S. Shprakh ◽  
V. Yu. Reshetnyak ◽  
O. V. Nesterova ◽  
I. N. Avertseva ◽  
...  
Keyword(s):  
Quantitative Analysis ◽  
Antitumor Activity ◽  
New Drugs ◽  
Antitumor Drugs ◽  
Pharmacokinetic Studies ◽  
Tumor Cell Death ◽  
Carbazole Derivatives ◽  
Pharmaceutical Substances ◽  
The Creation ◽  
Instrumental Methods

Introduction. Currently, more than 600 thousand people a year are affected by malignant tumors on the territory of the Russian Federation. Despite the large selection of antitumor drugs and the variety of mechanisms of their action, the effectiveness of existing drugs continues to be insufficient. The main disadvantages of most antitumor drugs are the emergence of tolerance to them of tumor cells, a limited range of action and high toxicity. In this regard, the creation of effective original domestic antitumor drugs still remains relevant. Among the numerous natural and synthetic heterocyclic compounds that exhibit antitumor activity, indolo[2,3-a]carbazole derivatives that can initiate various pathways of tumor cell death are of increasing interest. The main targets for their action are topoisomerases and protein kinases, which play an important role in the processes of replication, transcription, repair or recombination of deoxyribonucleic acid (DNA). Due to this, in addition to antitumor activity, this group of compounds shows antibacterial, аntiprotozoal and immunomodulatory activity, which makes them a very promising class of candidates for the creation of new drugs.Text. The purpose of this review is to discuss instrumental methods for qualitative and quantitative analysis of indolo[2,3-a]carbazole derivatives used in the world's leading pharmacopoeias. These methods can be used both in pharmacokinetic studies, and in the standardization of these compounds, in the form of pharmaceutical substances, or as part of drug forms.Conclusion. To further introduce a new group of antitumor drugs based on indole[2,3-a]carbazole derivatives into medical practice, a deep and thorough study of their physical and chemical properties is necessary. Justification and development of analysis methods allow us to develop methods applicable to pharmacokinetic studies, as well as to create regulatory documents for quality control and standardization of indolo[2,3-a] carbazole derivatives as pharmaceutical substances. A study of the literature that describes methods for analyzing indolo[2,3-a]carbazole derivatives indicates that spectrometric (infrared and ultraviolet spectrometry) and chromatographic (thin-layer chromatography and high-performance liquid chromatography) methods are most often used to determine the authenticity and quantitative analysis of these compounds.

scholarly journals Assessment of anticancer activity of Pulicaria undulata on hepatocellular carcinoma HepG2 cell line

Tumor Biology ◽  
2019 ◽  
Vol 41 (10) ◽  
pp. 101042831988008 ◽  
Author(s):  
Manal A Emam ◽  
Hemmat I Khattab ◽  
Marwa GA Hegazy
Keyword(s):  
Hepatocellular Carcinoma ◽  
Antitumor Activity ◽  
B Cell ◽  
Hepg2 Cell ◽  
Hepg2 Cells ◽  
Cell Lymphoma ◽  
B Cell Lymphoma ◽  
Antitumor Drugs ◽  
Phytochemical Analysis ◽  
Hepg2 Cell Line

Searching for new sources of safe nutraceuticals antitumor drugs is an important issue. Consequentially, this study designed to assess the antitumor activity of Pulicaria undulata extract in vitro in the treatment of hepatocellular carcinoma HepG2 cell line. Aerial parts of P. undulata plants were collected, used for phytochemical analysis, and assessed for anticancer activity. The antitumor activity was evaluated through studying the cell viability and apoptotic pathway. The gas chromatography–mass spectrometry phytochemical analysis revealed that P. undulata is a promising new source of several known antioxidant and antitumor compounds which could participate in drug development and exploration of alternative strategies to the harmful synthetic antitumor drugs. P. undulata stifled HepG2 cell viability in a concentration-dependent manner. Meanwhile, P. undulata tempted substantial apoptosis in HepG2 cells and enhanced the expression of miR-34a. However, the mRNA expression level of antiapoptotic B-cell lymphoma-2 was markedly decreased by P. undulata treatment. Moreover, P. undulata increased the protein expression of proapoptotic p53 and caspase 3/9 with reducing B-cell lymphoma-2 protein expression level. Thus, P. undulata induced apoptosis in the HepG2 cells by overexpression of miR-34a which regulates p53/B-cell lymphoma-2/caspases signaling pathway. These findings were well appreciated with morphological studies of cells treated with P. undulata. In conclusion, P. undulata could be a probable candidate agent for the initiation of cell apoptosis in HepG2 and thereby can serve as promising therapeutic agent for treatment of hepatocellular carcinoma which should attract further studies.

scholarly journals Cytotoxic and Antitumor Activity of some Coumarin Derivatives

2016 ◽  
Vol 11 (9) ◽  
pp. 1934578X1601100
Author(s):  
Hugo A. Garro ◽  
Guillermo F. Reta ◽  
Osvaldo J. Donadel ◽  
Carlos R. Pungitore
Keyword(s):  
Antitumor Activity ◽  
Tumor Cell ◽  
Cell Lines ◽  
Dna Polymerase ◽  
Antitumor Drugs ◽  
Tumor Cell Lines ◽  
Coumarin Derivatives ◽  
Lead Compound ◽  
Taq Dna Polymerase ◽  
Human Solid Tumor

Several natural and synthetic coumarins were assayed against different cancer cell lines. Four of them have shown cytotoxicity against a panel of three human solid tumor cell lines (HeLa, T-47D, and WiDr) and a clearly activity/hydrophobicity relationship. Compound 13 proved to be the most active product in all cell lines tested, with values of 8.0 (±0.38) μM against HeLa cells and also able to inhibit Taq DNA polymerase. This dual activity of 13 makes it a candidate to be considered as a “lead” compound in the search for novel antitumor drugs.

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