scholarly journals Biological activity of 3-(2-benzoxazol-5-yl)alanine derivatives

Amino Acids ◽  
2021 ◽  
Author(s):  
Katarzyna Guzow ◽  
Ewa Mulkiewicz ◽  
Michał Obuchowski ◽  
Wiesław Wiczk
Keyword(s):  
Biological Activity ◽  
Cancer Cells ◽  
Anticancer Agents ◽  
Multidrug Resistant ◽  
Biologically Active ◽  
New Drugs ◽  
Screening Tests ◽  
Chemistry Industry ◽  
Large Group ◽  
Gram Positive Bacteria

AbstractSearching for new drugs is still a challenge for science, mainly because of civilization development and globalization which promote the rapid spread of diseases, which is particularly dangerous in the case of infectious ones. Moreover, readily available already known antibiotics are often overused or misused, possibly contributing to the increase in the number of multidrug-resistant microorganisms. A consequence of this is the need for new structures of potential drugs. One of them is a benzoxazole moiety, a basic skeleton of a group of fluorescent heterocyclic compounds already widely used in chemistry, industry, and medicine, which is also present in naturally occurring biologically active compounds. Moreover, synthetic benzoxazoles are also biologically active. Considering all of that, a large group of non-proteinogenic amino acids based on 3-(2-benzoxazol-5-yl)alanine skeleton was studied in search for new antimicrobial and anticancer agents. Screening tests revealed that antibacterial potential of 41 compounds studied is not very high; however, they are selective acting only against Gram-positive bacteria (B. subtilis). Moreover, almost half of the studied compounds have antifungal properties, also against pathogens (C. albicans). Most of studied compounds are toxic to both normal and cancer cells. However, in a few cases, toxicity to normal cells is much lower than for cancer cells indicating these compounds as future anticancer agents. The research carried out on such a large group of compounds allowed to establish a structure–activity relationship which enables to select candidates for further modifications, necessary to improve their biological activity and obtain a new lead structure with potential for therapeutic use.

Biological Activity of Trans-Membrane Anion Carriers

2018 ◽  
Vol 25 (30) ◽  
pp. 3560-3576 ◽  
Author(s):  
Massimo Tosolini ◽  
Paolo Pengo ◽  
Paolo Tecilla
Keyword(s):  
Biological Activity ◽  
Membrane Transport ◽  
Anticancer Agents ◽  
Biological Effects ◽  
Structure Activity Relationship ◽  
New Drugs ◽  
Activity Relationship ◽  
Anion Channels ◽  
Cellular Homeostasis ◽  
Structure Activity

Natural and synthetic anionophores promote the trans-membrane transport of anions such as chloride and bicarbonate. This process may alter cellular homeostasis with possible effects on internal ions concentration and pH levels triggering several and diverse biological effects. In this article, an overview of the recent results on the study of aniontransporters, mainly acting with a carrier-type mechanism, is given with emphasis on the structure/activity relationship and on their biological activity as antibiotic and anticancer agents and in the development of new drugs for treating conditions derived from dysregulation of natural anion channels.

Oxazole-Based Compounds As Anticancer Agents

2020 ◽  
Vol 26 (41) ◽  
pp. 7337-7371 ◽  
Author(s):  
Maria A. Chiacchio ◽  
Giuseppe Lanza ◽  
Ugo Chiacchio ◽  
Salvatore V. Giofrè ◽  
Roberto Romeo ◽  
...  
Keyword(s):  
Cancer Research ◽  
Drug Discovery ◽  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Chemical Diversity ◽  
Biologically Active ◽  
New Drugs ◽  
The Core ◽  
Anti Cancer ◽  
Biologically Active Derivatives

: Heterocyclic compounds represent a significant target for anti-cancer research and drug discovery, due to their structural and chemical diversity. Oxazoles, with oxygen and nitrogen atoms present in the core structure, enable various types of interactions with different enzymes and receptors, favoring the discovery of new drugs. Aim of this review is to describe the most recent reports on the use of oxazole-based compounds in anticancer research, with reference to the newly discovered iso/oxazole-based drugs, to their synthesis and to the evaluation of the most biologically active derivatives. The corresponding dehydrogenated derivatives, i.e. iso/oxazolines and iso/oxazolidines, are also reported.

Isoselenocyanates: Synthesis and Their Use for Preparing Selenium-Based Heterocycles

Synthesis ◽  
2021 ◽  
Author(s):  
Stefan H. Bossmann ◽  
Raul Neri
Keyword(s):  
Biological Activity ◽  
Infectious Diseases ◽  
Cancer Cells ◽  
Multicomponent Reactions ◽  
Oxidative Cyclization ◽  
Biologically Active ◽  
Organoselenium Compounds ◽  
X Ray ◽  
Synthetic Work

AbstractIsoselenocyanates (ISCs) are a class of organoselenium compounds that have been recognized as potential chemotherapeutic and chemopreventative agents against cancer(s) and infectious diseases. ISC compounds are chemically analogous to their isosteric relatives, isothiocyanates (ITCs); however, they possess increased biological activity, such as enhanced cytotoxicity against cancer cells. ISCs not only serve as significant products, but also as precursors and essential intermediates for a variety of organoselenium compounds, such as selenium-containing heterocycles, which are biologically active. While syntheses of ISCs have become less difficult to accomplish, the syntheses of selenium-containing heterocycles are often difficult due to the use of highly toxic selenium reagents. Because of this, ISCs can serve as versatile reagents for the preparation of these heterocycles. In this review, the classical and recent syntheses of ISCs will be discussed, along with notable and recent synthetic work employing ISCs to access novel selenium-containing heterocycles.1 Introduction1.1 Selenium and Health2 Isoselenocyanates2.1 Preparation of Isoselenocyanates3 Selenium-Containing Heterocycles3.1 Notable Synthetic Work3.2 Recent Synthetic Work3.2.1 Synthesis of N-(3-Methyl-4-phenyl-3H-selenazol-2-ylidene)benzamide­ Derivatives3.2.2 Synthesis and X-ray Studies of Diverse Selenourea Derivatives3.2.3 Synthesis of Heteroarene-Fused [1,2,4]Thiadiazoles/Selenadiazoles via Iodine-Promoted [3+2] Oxidative Cyclization3.2.4 2-Amino-1,3-selenazole Derivatives via Base-Promoted Multicomponent Reactions4 Conclusion

Bacteriocins of Gram-positive bacteria having activity spectra extending beyond closely-related species

2019 ◽  
Vol 10 (3) ◽  
pp. 315-328 ◽  
Author(s):  
S.D. Todorov ◽  
B.D.G. de Melo Franco ◽  
J.R. Tagg
Keyword(s):  
Critical Points ◽  
Anticancer Agents ◽  
Multidrug Resistant ◽  
Food Preservation ◽  
Resistant Bacteria ◽  
Closely Related Species ◽  
Gram Positive Bacteria ◽  
Activity Spectrum ◽  
Novel Applications ◽  
Selection Of

Bacteriocins are bacterially-produced antimicrobial peptides that have killing activity principally against other relatively closely-related bacteria. Some bacteriocins of the lactic acid bacteria (LAB) have for many years been extensively applied in food biopreservation. However, especially during the last decade, a number of reports have appeared about unanticipated extensions to the generally rather narrow anti-bacterial activity spectrum of some of the LAB bacteriocins and novel applications have been proposed for bacteriocins ranging from controlling the growth of an increasingly-heterogeneous variety of pathogens, including Gram-negative multidrug resistant bacteria, viruses, yeasts, and in particular, difficult to control Mycobacterium spp., to their potential application as anticancer agents. How best can we assess this now rapidly-accumulating stream of reports on potential future applications of bacteriocins? Where is the line between realistic, science-based proposals and highly-speculative fiction and what are the ‘critical points’ that might help us to draw this line? In this review, we have attempted to analyse a selection of the presently-available data concerning relatively ‘unorthodox’ (i.e. beyond food preservation) applications of bacteriocins, and, by utilising our set of ‘critical points’, we endeavour to identify essential or/and missing information that appear crucial for success of the proposed applications.

scholarly journals Evaluation of the In Vitro Cytotoxic Activity of Ursolic Acid PLGA Nanoparticles against Pancreatic Ductal Adenocarcinoma Cell Lines

Materials ◽  
2021 ◽  
Vol 14 (17) ◽  
pp. 4917
Author(s):  
Adam Markowski ◽  
Paweł Migdał ◽  
Adrianna Zygmunt ◽  
Magdalena Zaremba-Czogalla ◽  
Jerzy Gubernator
Keyword(s):  
Biological Activity ◽  
Pancreatic Ductal Adenocarcinoma ◽  
Ursolic Acid ◽  
Water Solubility ◽  
Unmet Need ◽  
Plga Nanoparticles ◽  
Biologically Active ◽  
New Drugs ◽  
Ductal Adenocarcinoma ◽  
Pancreatic Cancer Cells

Among all the types of cancer, Pancreatic Ductal Adenocarcinoma remains one of the deadliest and hardest to fight and there is a critical unmet need for new drugs and therapies for its treatment. Naturally derived compounds, such as pentacyclic triterpenoids, have gathered attention because of their high cytotoxic potential towards pancreatic cancer cells, with a wide biological activity spectrum, with ursolic acid (UA) being one of the most interesting. However, due to its minimal water solubility, it is necessary to prepare a nanocarrier vehicle to aid in the delivery of this compound. Poly(lactic-co-glycolic acid) or PLGA polymeric nanocarriers are an essential tool for ursolic acid delivery and can overcome the lack in its biological activity observed after incorporating within liposomes. We prepared UA-PLGA nanoparticles with a PEG modification, to achieve a long circulation time, by using a nanoprecipitation method and subsequently performed an MTT cytotoxicity assay towards AsPC-1 and BxPC-3 cells, with TEM visualization of the nanoparticles and their cellular uptake. We established repeatable preparation procedures of the nanoparticles and achieved biologically active nanocarriers with an IC50 below 30 µM, with an appropriate size for intravenous dosage (around 140 nm), high sample homogeneity (below 0.2) and reasonable encapsulation efficiency (up to 50%). These results represent the first steps in the development of potentially effective PDAC therapies based on novel biologically active and promising triterpenoids.

scholarly journals New Synthetic Nitro-Pyrrolomycins as Promising Antibacterial and Anticancer Agents

Antibiotics ◽  
2020 ◽  
Vol 9 (6) ◽  
pp. 292 ◽  
Author(s):  
Maria Valeria Raimondi ◽  
Alessandro Presentato ◽  
Giovanna Li Petri ◽  
Miriam Buttacavoli ◽  
Agnese Ribaudo ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Biological Activity ◽  
Anticancer Agents ◽  
Mode Of Action ◽  
Biologically Active ◽  
Minimal Bactericidal Concentration ◽  
High Cytotoxicity ◽  
Pathogen Strains ◽  
Mcf 7

Pyrrolomycins (PMs) are polyhalogenated antibiotics known as powerful biologically active compounds, yet featuring high cytotoxicity. The present study reports the antibacterial and antitumoral properties of new chemically synthesized PMs, where the three positions of the pyrrolic nucleus were replaced by nitro groups, aiming to reduce their cytotoxicity while maintaining or even enhancing the biological activity. Indeed, the presence of the nitro substituent in diverse positions of the pyrrole determined an improvement of the minimal bactericidal concentration (MBC) against Gram-positive (i.e., Staphylococcus aureus) or -negative (i.e., Pseudomonas aeruginosa) pathogen strains as compared to the natural PM-C. Moreover, some new nitro-PMs were as active as or more than PM-C in inhibiting the proliferation of colon (HCT116) and breast (MCF 7) cancer cell lines and were less toxic towards normal epithelial (hTERT RPE-1) cells. Altogether, our findings contribute to increase the knowledge of the mode of action of these promising molecules and provide a basis for their rationale chemical or biological manipulation.

Chalcone derivatives and their activities against drug-resistant cancers: An overview

2020 ◽  
Vol 20 ◽  
Author(s):  
Jiaqi Xiao ◽  
Meixiang Gao ◽  
Qiang Diao ◽  
Feng Gao
Keyword(s):  
Drug Resistance ◽  
Multidrug Resistance ◽  
Cancer Cells ◽  
Anticancer Agents ◽  
Rational Design ◽  
Multidrug Resistant ◽  
Drug Resistant ◽  
Chalcone Derivatives ◽  
Potential Activity ◽  
Defensive Mechanisms

: Drug resistance including multidrug resistance resulting from different defensive mechanisms in cancer cells is the leading cause of the failure about the cancer therapy, making it an urgent need to develop more effective anticancer agents. Chalcones, widely distributed in nature, could act on diverse enzymes and receptors in cancer cells. Accordingly, chalcone derivatives possess potential activity against various cancers including drug-resistant even multidrug-resistant cancer. This review outlines the recent development of chalcone derivatives with potential activity against drug-resistant cancers covering articles published between 2010 and 2020, so as to facilitate further rational design of more effective candidate.

Biologically active secondary metabolites from Actinomycetes

2012 ◽  
Vol 7 (3) ◽  
pp. 373-390 ◽  
Author(s):  
Jolanta Solecka ◽  
Joanna Zajko ◽  
Magdalena Postek ◽  
Aleksandra Rajnisz
Keyword(s):  
Biological Activity ◽  
Secondary Metabolites ◽  
Chemical Structure ◽  
Multidrug Resistant ◽  
Biologically Active ◽  
Plant Roots ◽  
Bacterial Strains ◽  
Genus Streptomyces ◽  
Gram Negative ◽  
Potential Source

AbstractSecondary metabolites obtained from Actinomycetales provide a potential source of many novel compounds with antibacterial, antitumour, antifungal, antiviral, antiparasitic and other properties. The majority of these compounds are widely used as medicines for combating multidrug-resistant Gram-positive and Gram-negative bacterial strains. Members of the genus Streptomyces are profile producers of previously-known secondary metabolites. Actinomycetes have been isolated from terrestrial soils, from the rhizospheres of plant roots, and recently from marine sediments. This review demonstrates the diversity of secondary metabolites produced by actinomycete strains with respect to their chemical structure, biological activity and origin. On the basis of this diversity, this review concludes that the discovery of new bioactive compounds will continue to pose a great challenge for scientists.

scholarly journals Chlorophyll and Chlorophyll Derivatives Interfere with Multi-Drug Resistant Cancer Cells and Bacteria

Molecules ◽  
2019 ◽  
Vol 24 (16) ◽  
pp. 2968 ◽  
Author(s):  
Erjia Wang ◽  
Markus Santhosh Braun ◽  
Michael Wink
Keyword(s):  
Cancer Cells ◽  
Methicillin Resistant Staphylococcus Aureus ◽  
Human Cancer ◽  
Efflux Pumps ◽  
Multidrug Resistant ◽  
New Drugs ◽  
Human Cancer Cells ◽  
Significant Reversal ◽  
Challenging Tasks ◽  
Chlorophyll Derivatives

Multidrug resistance (MDR) causes challenging tasks in medicine. Human cancer cells, as well as microorganisms, can acquire multiresistance due to the up-regulation of efflux pumps (ABC transporters) and are difficult to treat. Here, we evaluated the effects of chlorophyll, the most abundant pigment on the globe, and its derivative, pheophytin, on cancer cells and methicillin-resistant Staphylococcus aureus (MRSA). We found that both substances have significant reversal effects on multidrug-resistant CEM/ADR5000 cells (RRpheophytin = 3.13, combination index (CI)pheophytin = 0.438; RRchlorophyll = 2.72, CIchlorophyll < 0.407), but not on drug-sensitive CCRF-CEM cells when used in combination with doxorubicin. This indicates that the porphyrins could interact with efflux pumps. Strong synergism was also observed in antimicrobial tests against MRSA when combining ethidium bromide with chlorophyll (FICI = 0.08). As there is a strong need for new drugs in order to reliably treat MDR cells, our research provides potential candidates for further investigation.

scholarly journals Recent Advances in Repurposing Disulfiram and Disulfiram Derivatives as Copper-Dependent Anticancer Agents

2021 ◽  
Vol 8 ◽  
Author(s):  
Vinodh Kannappan ◽  
Misha Ali ◽  
Benjamin Small ◽  
Gowtham Rajendran ◽  
Salena Elzhenni ◽  
...  
Keyword(s):  
Clinical Trials ◽  
Cancer Cells ◽  
Cancer Progression ◽  
Anticancer Agents ◽  
Molecular Targets ◽  
Cancer Therapeutics ◽  
New Drugs ◽  
Cancer Clinical Trials ◽  
Anticancer Efficacy ◽  
Wide Range

Copper (Cu) plays a pivotal role in cancer progression by acting as a co-factor that regulates the activity of many enzymes and structural proteins in cancer cells. Therefore, Cu-based complexes have been investigated as novel anticancer metallodrugs and are considered as a complementary strategy for currently used platinum agents with undesirable general toxicity. Due to the high failure rate and increased cost of new drugs, there is a global drive towards the repositioning of known drugs for cancer treatment in recent years. Disulfiram (DSF) is a first-line antialcoholism drug used in clinics for more than 65 yr. In combination with Cu, it has shown great potential as an anticancer drug by targeting a wide range of cancers. The reaction between DSF and Cu ions forms a copper diethyldithiocarbamate complex (Cu(DDC)2 also known as CuET) which is the active, potent anticancer ingredient through inhibition of NF-κB and ubiquitin-proteasome system as well as alteration of the intracellular reactive oxygen species (ROS). Importantly, DSF/Cu inhibits several molecular targets related to drug resistance, stemness, angiogenesis and metastasis and is thus considered as a novel strategy for overcoming tumour recurrence and relapse in patients. Despite its excellent anticancer efficacy, DSF has proven unsuccessful in several cancer clinical trials. This is likely due to the poor stability, rapid metabolism and/or short plasma half-life of the currently used oral version of DSF and the inability to form Cu(DDC)2 at relevant concentrations in tumour tissues. Here, we summarize the scientific rationale, molecular targets, and mechanisms of action of DSF/Cu in cancer cells and the outcomes of oral DSF ± Cu in cancer clinical trials. We will focus on the novel insights on harnessing the immune system and hypoxic microenvironment using DSF/Cu complex and discuss the emerging delivery strategies that can overcome the shortcomings of DSF-based anticancer therapies and provide opportunities for translation of DSF/Cu or its Cu(DDC)2 complex into cancer therapeutics.

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