scholarly journals Review of the Synthesis and Anticancer Properties of Pyrazolo[4,3-e][1,2,4]triazine Derivatives

Molecules ◽  
2020 ◽  
Vol 25 (17) ◽  
pp. 3948
Author(s):  
Zofia Bernat ◽  
Anna Szymanowska ◽  
Mateusz Kciuk ◽  
Katarzyna Kotwica-Mojzych ◽  
Mariusz Mojzych

This review focuses on the cytotoxic effect of new synthetic pyrazolo[4,3-e][1,2,4]triazine derivatives against different tumor cell lines. Some annulated pyrazolotriazines i.e., pyrazolo[4,3-e][1,2,4]triazolo[4,3-b][1,2,4]triazines and pyrazolo[4,3-e]tetrazolo[1,5-b][1,2,4]triazine demonstrated significant broad cytotoxic activity in micromolar range concentration, which could have excellent potential to be new candidate therapeutic agents in cancer chemotherapy.

2012 ◽  
Vol 2012 ◽  
pp. 1-8 ◽  
Author(s):  
Patrícia Mathias Döll-Boscardin ◽  
Adilson Sartoratto ◽  
Beatriz Helena Lameiro de Noronha Sales Maia ◽  
Josiane Padilha de Paula ◽  
Tomoe Nakashima ◽  
...  

EucalyptusL. is traditionally used for many medicinal purposes. In particular, someEucalyptusspecies have currently shown cytotoxic properties. Local Brazilian communities have used leaves ofE. benthamiias a herbal remedy for various diseases, including cancer. Considering the lack of available data for supporting this cytotoxic effect, the goal of this paper was to study thein vitrocytotoxic potential of the essential oils from young and adult leaves ofE. benthamiiand some related terpenes (α-pinene, terpinen-4-ol, andγ-terpinene) on Jurkat, J774A.1 and HeLa cells lines. Regarding the cytotoxic activity based on MTT assay, the essential oils showed improved results thanα-pinene andγ-terpinene, particularly for Jurkat and HeLa cell lines. Terpinen-4-ol revealed a cytotoxic effect against Jurkat cells similar to that observed for volatile oils. The results of LDH activity indicated that cytotoxic activity of samples against Jurkat cells probably involved cell death by apoptosis. The decrease of cell DNA content was demonstrated due to inhibition of Jurkat cells proliferation by samples as a result of cytotoxicity. In general, the essential oils from young and adult leaves ofE. benthamiipresented cytotoxicity against the investigated tumor cell lines which confirms their antitumor potential.


Proceedings ◽  
2019 ◽  
Vol 22 (1) ◽  
pp. 4
Author(s):  
Eugene Rogozhin ◽  
Vera Sadykova

Soil fungi are known to produce and secrete antibiotics with a strong antimicrobial effect towards eukaryotic organisms. In many occasions, these compounds belong to peptides that are products of non-ribosomal biosynthesis and are called peptaibols. Many peptaibols are cytotoxic and some of them suppress tumor cell lines much better than normal cells by inducing calcium-mediated apoptosis. The main antimicrobial lipoaminopeptaibol—emericellipsin A—isolated from the fungus Emericellopsis alkalina strain VKPM F-1428, which demonstrates promising antifungal activity against different fungal taxons,has been found to exhibit selective cytotoxic activity against HepG2 and Hela cell lines (EC50 2.8 and 0.5 μM, respectively) in MTT assays in vitro. This result corresponds to the standard antitumor antibiotic doxorubicin, which has an EC50 value of 440 nM. In a fibroblast toxicity test, emericellipsin A exhibited less cytotoxic activity than doxorubicin (EC50 14 and 0.34 μM, respectively). Therefore, it is less toxic to normal cells than doxirubicin (~40 times), but it yields a more potent cytotoxic effect on tumor cell lines. That is why emericellipsin A can be considered for future more detailed investigations to be an effective antitumor substance.


2013 ◽  
Vol 16 (1) ◽  
pp. 137-142
Author(s):  
Farooq I. Mohammed ◽  
◽  
Farah T. Abdullah ◽  
Shaimaa Y. Abdulfttah ◽  
◽  
...  

2019 ◽  
Vol 18 (4) ◽  
pp. 1051-1100
Author(s):  
Lenka Molčanová ◽  
Dominika Janošíková ◽  
Stefano Dall´Acqua ◽  
Karel Šmejkal

Toxicon ◽  
2012 ◽  
Vol 59 (7-8) ◽  
pp. 667-671 ◽  
Author(s):  
Erika S. Nunes ◽  
Mary A.A. Souza ◽  
Antônio F.M. Vaz ◽  
Teresinha G. Silva ◽  
Jaciana S. Aguiar ◽  
...  

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 ◽  
...  

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.


1989 ◽  
Vol 42 (12) ◽  
pp. 1877-1878 ◽  
Author(s):  
SHIGETAKA ISHII ◽  
MIEKO NAGASAWA ◽  
YUKO KARIYA ◽  
HARUO YAMAMOTO

2013 ◽  
Vol 2013 ◽  
pp. 1-12 ◽  
Author(s):  
Wilfredo Hernández ◽  
Juan Paz ◽  
Fernando Carrasco ◽  
Abraham Vaisberg ◽  
Evgenia Spodine ◽  
...  

The palladium(II) bis-chelate complexes of the type [Pd(TSC1-5)2] (6–10), with their corresponding ligands 4-phenyl-1-(acetone)-thiosemicarbazone, HTSC1(1), 4-phenyl-1-(2′-chloro-benzaldehyde)-thiosemicarbazone, HTSC2(2), 4-phenyl-1-(3′-hydroxy-benzaldehyde)-thiosemicarbazone, HTSC3(3), 4-phenyl-1-(2′-naphthaldehyde)-thiosemicarbazone, HTSC4(4), and 4-phenyl-1-(1′-nitro-2′-naphthaldehyde)-thiosemicarbazone, HTSC5(5), were synthesized and characterized by elemental analysis and spectroscopic techniques (IR and1H- and13C-NMR). The molecular structure of HTSC3, HTSC4, and [Pd(TSC1)2] (6) have been determined by single crystal X-ray crystallography. Complex6shows a square planar geometry with two deprotonated ligands coordinated toPdIIthrough the azomethine nitrogen and thione sulfur atoms in acisarrangement. Thein vitrocytotoxic activity measurements indicate that the palladium(II) complexes (IC50=0.01–9.87 μM) exhibited higher antiproliferative activity than their free ligands (IC50=23.48–70.86 and >250 μM) against different types of human tumor cell lines. Among all the studied palladium(II) complexes, the [Pd(TSC3)2] (8) complex exhibited high antitumor activity on the DU145 prostate carcinoma and K562 chronic myelogenous leukemia cells, with low values of the inhibitory concentration (0.01 and 0.02 μM, resp.).Corrigendum to “Synthesis and Characterization of New Palladium(II) Thiosemicarbazone Complexes and Their Cytotoxic Activity against Various Human Tumor Cell Lines”


1997 ◽  
Vol 7 (23) ◽  
pp. 2945-2950 ◽  
Author(s):  
Axel Monsees ◽  
Sabine Laschat ◽  
Marc Hotfilder ◽  
Johannes Wolff ◽  
Klaus Bergander ◽  
...  

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