antitumor compounds
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Molecules ◽  
2021 ◽  
Vol 26 (24) ◽  
pp. 7600
Author(s):  
Iogann Tolbatov ◽  
Alessandro Marrone ◽  
Cecilia Coletti ◽  
Nazzareno Re

Owing to the growing hardware capabilities and the enhancing efficacy of computational methodologies, computational chemistry approaches have constantly become more important in the development of novel anticancer metallodrugs. Besides traditional Pt-based drugs, inorganic and organometallic complexes of other transition metals are showing increasing potential in the treatment of cancer. Among them, Au(I)- and Au(III)-based compounds are promising candidates due to the strong affinity of Au(I) cations to cysteine and selenocysteine side chains of the protein residues and to Au(III) complexes being more labile and prone to the reduction to either Au(I) or Au(0) in the physiological milieu. A correct prediction of metal complexes’ properties and of their bonding interactions with potential ligands requires QM computations, usually at the ab initio or DFT level. However, MM, MD, and docking approaches can also give useful information on their binding site on large biomolecular targets, such as proteins or DNA, provided a careful parametrization of the metal force field is employed. In this review, we provide an overview of the recent computational studies of Au(I) and Au(III) antitumor compounds and of their interactions with biomolecular targets, such as sulfur- and selenium-containing enzymes, like glutathione reductases, glutathione peroxidase, glutathione-S-transferase, cysteine protease, thioredoxin reductase and poly (ADP-ribose) polymerase 1.


2021 ◽  
Vol 12 (4) ◽  
pp. 840-846
Author(s):  
Paris Laskaris ◽  
Amalia D. Karagouni

Bacteria of the genus Streptomyces produce a very large number of secondary metabolites, many of which are of vital importance to modern medicine. There is great interest in the discovery of novel pharmaceutical compounds derived from strepomycetes, since novel antibiotics, anticancer and compounds for treating other conditions are urgently needed. Greece, as proven by recent research, possesses microbial reservoirs with a high diversity of Streptomyces populations, which provide a rich pool of strains with potential pharmaceutical value. This review examines the compounds of pharmaceutical interest that have been derived from Greek Streptomyces isolates. The compounds reported in the literature include antibiotics, antitumor compounds, biofilm inhibitors, antiparasitics, bacterial toxin production inhibitors and antioxidants. The streptomycete biodiversity of Greek environments remains relatively unexamined and is therefore a very promising resource for potential novel pharmaceuticals.


Author(s):  
Anindita Ghosh ◽  
Chinmay Kumar Panda

: Bladder cancer carries a poor prognosis and has proven resistance to chemotherapy. Pentacyclic Triterpenoid Acids (PTAs) are natural bioactive compounds that have a well-known impact on cancer research because of their cytotoxic and chemopreventive activities. This review focuses on bladder cancer which can no longer be successfully treated by DNA damaging drugs. Unlike most of the existing drugs against bladder cancer, PTAs are non-toxic to normal cells. Collecting findings from both in vitro and in vivo studies, it has been concluded that PTAs may serve as promising agents in future bladder cancer therapy. In this review, the roles of various PTAs in bladder cancer have been explored, and their mechanisms of action in the treatment of bladder cancer have been described. Specific PTAs have been shortlisted from each of the chief skeletons of pentacyclic triterpenoids, which could be effective against bladder cancer because of their mode of action. This review thereby throws light on the multi targets and mechanisms of PTAs, which are responsible for their selective anticancer effects and provides guidelines for further research and development of new natural antitumor compounds.


Molecules ◽  
2021 ◽  
Vol 26 (20) ◽  
pp. 6262
Author(s):  
Jolanta Kulesza ◽  
Monika Pawłowska ◽  
Ewa Augustin

The culture of 3D spheroids is a promising tool in drug development and testing. Recently, we synthesized a new group of compounds, unsymmetrical bisacridines (UAs), which exhibit high cytotoxicity against various human cell lines and antitumor potency against several xenografts. Here, we describe the ability of four UAs—C-2028, C-2041, C-2045, and C-2053—to influence the growth of HCT116 and H460 spheres and the viability of HCT116 cells in 3D culture compared with that in 2D standard monolayer culture. Spheroids were generated using ultra-low-attachment plates. The morphology and diameters of the obtained spheroids and those treated with UAs were observed and measured under the microscope. The viability of cells exposed to UAs at different concentrations and for different incubation times in 2D and 3D cultures was assessed using 7-AAD staining. All UAs managed to significantly inhibit the growth of HCT116 and H460 spheroids. C-2045 and C-2053 caused the death of the largest population of HCT116 spheroid cells. Although C-2041 seemed to be the most effective in the 2D monolayer experiments, in 3D conditions, it turned out to be the weakest compound. The 3D spheroid culture seems to be a suitable method to examine the efficiency of new antitumor compounds, such as unsymmetrical bisacridines.


Author(s):  
Meilin Mu ◽  
Jiuyu Zhan ◽  
Xiaohan Dai ◽  
Hongwei Gao

Author(s):  
Carrasco-Reinado, Rafael ◽  
Escobar-Niño, Almudena ◽  
Fernández-Acero, Francisco Javier

Molecules ◽  
2021 ◽  
Vol 26 (10) ◽  
pp. 2926
Author(s):  
Alexandra G. Durán ◽  
M. Teresa Gutiérrez ◽  
Francisco J. R. Mejías ◽  
José M. G. Molinillo ◽  
Francisco A. Macías

Annona cherimola Mill., or the custard apple, is one of the species belonging to the Annonaceae family, is widely used in traditional medicine, and has been reported to be a valuable source of bioactive compounds. A unique class of secondary metabolites derived from this family are Annonaceous acetogenins, lipophilic polyketides considered to be amongst the most potent antitumor compounds. This review provides an overview of the chemical diversity, isolation procedures, bioactivity, modes of application and synthetic derivatives of acetogenins from A. cherimola Mill.


2021 ◽  
Vol 10 (10) ◽  
Author(s):  
Shu Zhao ◽  
David Koffi ◽  
Jean-Paul Latge ◽  
Karidia Sylla ◽  
John G. Gibbons

ABSTRACT Aspergillus aculeatinus is an industrially important species of Aspergillus section Nigri capable of producing bioactive, antibiotic, and antitumor compounds. We sequenced the genome of a strain of A. aculeatinus that was isolated from the interior of a housing complex in Abidjan, Ivory Coast.


Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1521
Author(s):  
Micael Rodrigues Cunha ◽  
Maurício Temotheo Tavares ◽  
Thais Batista Fernandes ◽  
Roberto Parise-Filho

Piper, Capsicum, and Pimenta are the main genera of peppers consumed worldwide. The traditional use of peppers by either ancient civilizations or modern societies has raised interest in their biological applications, including cytotoxic and antiproliferative effects. Cellular responses upon treatment with isolated pepper-derived compounds involve mechanisms of cell death, especially through proapoptotic stimuli in tumorigenic cells. In this review, we highlight naturally occurring secondary metabolites of peppers with cytotoxic effects on cancer cell lines. Available mechanisms of cell death, as well as the development of analogues, are also discussed.


2021 ◽  
Vol 2 (1(82)) ◽  
pp. 72-76
Author(s):  
N. Ovchinnikova ◽  
I. Eremenko

Development of the new methods for drug production is impossible without reliance on the novel and unorthodox approaches to the synthesis of heterocyclic complexes and compounds.The method is based on the study of new aspects of the of two types of behavior of the coordinated molecules in reaction - their ability to insert into the same transition metal-halogen bond, and their ability to form the unusual heterocyclic ligands, or even molecules after leaving the complex’s coordination sphere. This will make it possible not only to synthesize the already-known compounds under milder conditions, but to also obtain new ones as products of such mixed condensation reactions. On the one hand, this opens up new possibilities for designing and performing the intraspherical "stitching" of ligands and their synthesis with high efficiency and selectivity.  On the other hand, these reactions can be considered a significant contribution to the fundamental coordination chemistry in terms of illustration of the new modalities of the mutual influence of ligands, namely their ability to stimulate each other for a mutual insertion, and sheds light on the mechanisms of the intraspheric condensation. Oxadiazine derivatives, just like the derivatives of triazine we synthesized and reported previously, could become a foundation for the generation of biologically-active compounds, often containing heterocyclic fragments and frequently used for the treatment of malignant tumors. It can be expected that the developed method will find use in the synthesis of the new classes of potential antitumor compounds. We have previously found that organic isocyanate not only themselves insert into M-Hal bond, but can also activate the insertion of acetonitrile, the resulting heteromolecular chain of inserted molecules being composed of two MeNCO and one MeCN fragments. Such a structure of this complexes was confirmed be synthesis of striazine derivatives on their base. In this work was to determine optimum condition for the insertion of ethyl isocyanate with acetone into niobium-chlorine bond, as well as their subsequent mixed co-cyclization with obtaining of oxadiazine derivative.


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