scholarly journals Schiff Base Metal Complexes as Anticancer Agents

2019 ◽  
Vol 31 (3) ◽  
pp. 493-504 ◽  
Author(s):  
G. Sridevi ◽  
S. Arul Antony ◽  
R. Angayarkani
Keyword(s):  
Schiff Base ◽  
Anticancer Agents ◽  
Anticancer Agent ◽  
Antitumor Agents ◽  
Transition Metal Complex ◽  
Bioinorganic Chemistry ◽  
Structural Data ◽  
Ligand Substitution ◽  
Schiff Base Metal Complexes

Cutting-edge practices in bioinorganic chemistry are pivotal for enhancing the layout of compounds to lessen poisonous facet effect and recognize their mechanism of action. A powerful anticancer agent should own inherent, inhibitory property and also delivery, dosage and residence time in vivo. Organic function and conformation of mutated gene may be altered by way of binding of metal ions. Upswing of activities counting on the structural data, intending in enhancing and growing different forms of metal based compounds, continuous seek of extra metal based compounds have been synthesized via revamping the prevailing chemical shape via ligand substitution. The prevailing paper addresses the trendy development in the design of novel antitumor agents primarily based on transition metal complex via highlighting the near dating among their structural alternatives and cytotoxic ability.

Vitamin D as potential therapeutic anticancer agent

2018 ◽  
pp. 1-3
Keyword(s):  
Vitamin D ◽  
Anticancer Activity ◽  
Anticancer Agent ◽  
Antitumor Agents ◽  
Metastatic Potential ◽  
Anticancer Properties ◽  
Chemotherapy Agents

The role of vitamin D is implicated in carcinogenesis through numerous biological processes like induction of apoptosis, modulation of immune system inhibition of inflammation and cell proliferation and promotion of cell differentiation. Its use as additional adjuvant drug with cancer treatment may be novel combination for improved outcome of different cancers. Numerous preclinical, epidemiological and clinical studies support the role of vitamin D as an anticancer agent. Anticancer properties of vitamin D have been studied widely (both in vivo and in vitro) among various cancers and found to have promising results. There are considerable data that indicate synergistic potential of calcitriol and antitumor agents. Possible mechanisms for modulatory anticancer activity of vitamin D include its antiproliferative, prodifferentiating, and anti-angiogenic and apoptic properties. Calcitriol reduces invasiveness and metastatic potential of many cancer cells by inhibiting angiogenesis and regulating expression of the key molecules involved in invasion and metastasis. Anticancer activity of vitamin D is synergistic or additive with the antineoplastic actions of several drugs including cytotoxic chemotherapy agents like paclitaxel, docetaxel, platinum base compounds and mitoxantrone. Benefits of addition of vitamin D should be weighed against the risk of its toxicity.

scholarly journals Diarylureas as Antitumor Agents

2021 ◽  
Vol 11 (1) ◽  
pp. 374
Author(s):  
Alessia Catalano ◽  
Domenico Iacopetta ◽  
Maria Stefania Sinicropi ◽  
Carlo Franchini
Keyword(s):  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Anticancer Agent ◽  
Kinase Inhibitors ◽  
Antitumor Agents ◽  
Serine Threonine Kinase ◽  
Threonine Kinase ◽  
The Past ◽  
To Come ◽  
Come Into The Market

The diarylurea is a scaffold of great importance in medicinal chemistry as it is present in numerous heterocyclic compounds with antithrombotic, antimalarial, antibacterial, and anti-inflammatory properties. Some diarylureas, serine-threonine kinase or tyrosine kinase inhibitors, were recently reported in literature. The first to come into the market as an anticancer agent was sorafenib, followed by some others. In this review, we survey progress over the past 10 years in the development of new diarylureas as anticancer agents.

scholarly journals Repurposing Tranexamic Acid as an Anticancer Agent

2021 ◽  
Author(s):  
Mary E Law ◽  
Bradley J Davis ◽  
Amanda F Ghilardi ◽  
Elham Yaaghubi ◽  
Zaafir M Dulloo ◽  
...  
Keyword(s):  
Tranexamic Acid ◽  
Anticancer Agents ◽  
Intracellular Signaling ◽  
Anticancer Agent ◽  
Lead Compounds ◽  
Intracellular Signaling Pathways ◽  
Multiple Processes ◽  
Broad Array

Tranexamic Acid (TA) is a clinically used antifibrinolytic that acts as a lysine mimetic to block binding of Plasminogen with Plasminogen activators, preventing conversion of Plasminogen to its proteolytically activated form, Plasmin. Previous studies suggested that TA may exhibit anticancer activity by blockade of extracellular Plasmin formation. Plasmin-mediated cleavage of the CDCP1 protein may increase its oncogenic functions through several downstream pathways. Results presented herein demonstrate that TA blocks Plasmin-mediated excision of the extracellular domain of the oncoprotein CDCP1. In vitro studies indicate that TA reduces the viability of a broad array of human and murine cancer cell lines, and breast tumor growth studies demonstrate that TA reduces cancer growth in vivo. Based on the ability of TA to mimic lysine and arginine, we hypothesized that TA may perturb multiple processes that involve Lys/Arg-rich protein sequences, and that TA may alter intracellular signaling pathways in addition to blocking extracellular Plasmin production. Indeed, TA-mediated suppression of tumor cell viability is associated with multiple biochemical actions, including inhibition of protein synthesis, reduced activating phosphorylation of STAT3 and S6K1, decreased expression of the MYC oncoprotein, and suppression of Lys acetylation. These findings suggest that TA or TA analogs may serve as lead compounds and inspire the production of new classes of anticancer agents that function by mimicking Lys and Arg.

Novel Thiazine Substituted 9-Anilinoacridines: Synthesis, Antitumour Activity and Structure Activity Relationships

2019 ◽  
Vol 19 (11) ◽  
pp. 1350-1358 ◽  
Author(s):  
R. Kalirajan ◽  
K. Gaurav ◽  
A. Pandiselvi ◽  
B. Gowramma ◽  
S. Sankar
Keyword(s):  
Cell Lines ◽  
Anticancer Agents ◽  
Antitumor Agents ◽  
Antitumour Activity ◽  
Human Tumor ◽  
Cytotoxic Activities ◽  
Anti Tumour Activity ◽  
Tumour Activity

Background: 9-anilinoacridines are acting as DNA-intercalating agents which plays an important role as antitumor drugs, due to their anti-proliferative properties. Some anticancer agents contain 9- anilinoacridines such as amsacrine (m-AMSA), and nitracrine (Ledakrine) have been already developed. Methods: In this study, novel 9-anilinoacridines substituted with thiazines 4a-r were designed, synthesized, characterized by physical and spectral data and their cytotoxic activities against DLA cell lines were evaluated. Results: Among those compounds, 4b, c, e, g, i, j, k, m, o, p, q, r exhibited significant short term in vitro cytotoxic activity against Daltons lymphoma ascites (DLA) cells with CTC50 value of 0.18 to 0.31μM. The compounds 4b, c, e, g, i, j, k, m, o, p, q, r are also exhibited significant long term in vitro anti-tumour activity against human tumor cell lines, HEp-2 (laryngeal epithelial carcinoma) by Sulforhodamine B assay with CTC50 value of 0.20 to 0.39μM. The compounds 4b, i, j exhibited significant in vivo antitumor activity with % Increase in Life Span (ILS) 48-82%. Conclusion: Results obtained in this study clearly demonstrated that many of the thiazine substituted 9- anilinoacridines exert interesting anti-tumour activity. The compounds 4b, i, j have significant anti-tumour activity and useful drugs after further refinement. The above derivatives will encourage to design future antitumor agents with high therapeutic potentials.

Novel Hybrid Compound 4-[(E)-2-phenylethenesulfonamido]-N-hydroxybutanamide with Antimetastatic and Cytotoxic Action: Synthesis and Anticancer Screening

2019 ◽  
Vol 18 (10) ◽  
pp. 1495-1504 ◽  
Author(s):  
Yurii L. Zborovskii ◽  
Viktor V. Orysyk ◽  
Iuliia Golovynska ◽  
Olena I. Dzhus ◽  
Liudmyla V. Garmanchuk ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Antitumor Agents ◽  
Morphological Properties ◽  
Cytotoxic Action ◽  
Adhesive Properties ◽  
Hybrid Compound ◽  
Antiproliferative Agent ◽  
High Fraction

Background: One of the most promising strategies to develop multi-targeted anticancer therapeutics is to introduce to the structure of a potential drug two or more pharmacophores (functional groups or structural fragments), which have antiproliferative, proapoptotic or antimetastatic properties acting via different mechanisms. Objective: To design, synthesize and perform screening of a novel hybrid anticancer compound. Method: A novel hybrid compound 4-[(E)-2-phenylethenesulfonamido]-N-hydroxybutanamide, combining butanehydroxamate and styrenesulfonamide moieties, was designed, synthesized and investigated as a potent antimetastatic and antiproliferative agent. The structure and purity of the synthesized compound were confirmed by 1H NMR, 13C NMR, LC/MS spectroscopy and elemental analysis. The compound was screened for the anticancer activity in vitro against HeLa and in vivo against Lewis lung carcinoma tumor, using an antitumor metalloenzyme inhibitor GM6001 (Ilomastat, Galardin) and Pifithrin-μ as control anticancer agents. Results: It was found that the application of our compound resulted in a high fraction of apoptotic cells in the cell population, along with disruption in the cell cycle profile manifested as arrest of proliferative phases. Furthermore, changes of the morphological properties (i.e., an enhancement of adhesive properties and reduction of the nuclear-to-cytoplasm ratio) were found. The in vivo screening revealed that the compound significantly inhibited the metastasizing process that was manifested by a reduction in the number and volume of metastases. Conclusions: The obtained results demonstrate that our compound can serve as a base for further structure optimization in order to design new highly-effective antimetastatic and antitumor agents.

TISSUE CULTURE AND THE STUDY OF ANTICANCER AGENTS

1966 ◽  
Vol 44 (2) ◽  
pp. 339-343 ◽  
Author(s):  
Susan Tolnai
Keyword(s):  
Fatty Acids ◽  
Tumor Cells ◽  
Anticancer Agents ◽  
Antitumor Agents ◽  
Unsaturated Fatty Acids ◽  
Ascites Tumor ◽  
Mouse Tumors ◽  
Arachidonic Acids

In a quest for potential antitumor agents, more than 100 fatty acids and their derivatives were tested against transplantable mouse tumors with both in vivo and in vitro methods. Three compounds, 2,3-decenoic acid, linoleic acid, and linolenic acid, were found to arrest the growth of three types of ascites tumor cells, while 2-nonenoic, 10-undecenoic, oleic, and arachidonic acids were effective to a varying degree. The cytotoxic effects of these unsaturated fatty acids on monolayer cultures of Ehrlich ascites tumor cells and of normal mouse embryos were evaluated in experiments in which graded concentrations of the test materials incorporated in the culture medium were used.

scholarly journals Novel selective anticancer agents based on Sn and Au complexes. Mini-review

2020 ◽  
Vol 92 (8) ◽  
pp. 1201-1216
Author(s):  
Elena R. Milaeva ◽  
Dmitry B. Shpakovsky ◽  
Yulia A. Gracheva ◽  
Taisiya A. Antonenko ◽  
Tatyana D. Ksenofontova ◽  
...  
Keyword(s):  
Side Effects ◽  
Anticancer Agents ◽  
Antitumor Agents ◽  
Inorganic Compounds ◽  
Acquired Resistance ◽  
Cytotoxic Action ◽  
Mitochondrial Potential ◽  
Anti Cancer ◽  
Gold Compounds

AbstractCancer is one of the most common causes of death in modern medicine. Molecular design of novel substances with pharmacological activity is one of the goals of medicinal inorganic chemistry. Platinum complexes are widely used in the treatment of cancer, despite high efficacy their use is limited by side effects, as well as primary or acquired resistance. In this regard, the search for novel metal-containing antitumor compounds is underway. Organotins and gold compounds are promising pharmacological agents with anti-cancer properties. The introduction of protective antioxidant fragments into inorganic compounds molecules is a way to reduce the side effects of anti-cancer drugs on healthy cells. 2,6-dialkylphenols belonging to vitamin E (α-tocopherol) mimetics are widely used as antioxidants and stabilizers. The properties of Ph3SnCl (Sn-I), Ph3PAuCl (Au-I) and complexes Ph3SnSR (Sn-II) and Ph3PAuSR (Au-II) based on 2,6-di-tert-butyl-4-mercaptophenol (RSH) as radical scavengers and reducing agents were studied in model reactions. For Sn-II and Au-II the comparative study of cytotoxic action was made and the IC50 values on different cancer cell lines were found to be depended on the nature of metal. In general, Sn(IV) complexes possessed higher cytotoxicity than Au(I) complexes. In order to clarify the mechanism of cytotoxic mode of action the effect of compounds on Fe3+-induced lipid peroxidation, mitochondrial potential and mitochondrial permeability, cell cycle and induction of apoptosis was studied. Organotin compounds can bind tubulin SH-groups and inhibit its polymerization by a dose-dependent mechanism, whereas gold compounds inhibit Thioredoxin reductase (TrxR). In vivo experiments on acute toxicity of Sn-II and Au-II proved their moderate toxic action that opens prospects for the further study as antitumor agents.

scholarly journals Repurposing Tranexamic Acid as an Anticancer Agent

2022 ◽  
Vol 12 ◽  
Author(s):  
Mary E. Law ◽  
Bradley J. Davis ◽  
Amanda F. Ghilardi ◽  
Elham Yaaghubi ◽  
Zaafir M. Dulloo ◽  
...  
Keyword(s):  
Tranexamic Acid ◽  
Anticancer Agents ◽  
Intracellular Signaling ◽  
Anticancer Agent ◽  
Lead Compounds ◽  
Intracellular Signaling Pathways ◽  
Multiple Processes ◽  
Broad Array

Tranexamic Acid (TA) is a clinically used antifibrinolytic agent that acts as a Lys mimetic to block binding of Plasminogen with Plasminogen activators, preventing conversion of Plasminogen to its proteolytically activated form, Plasmin. Previous studies suggested that TA may exhibit anticancer activity by blockade of extracellular Plasmin formation. Plasmin-mediated cleavage of the CDCP1 protein may increase its oncogenic functions through several downstream pathways. Results presented herein demonstrate that TA blocks Plasmin-mediated excision of the extracellular domain of the oncoprotein CDCP1. In vitro studies indicate that TA reduces the viability of a broad array of human and murine cancer cell lines, and breast tumor growth studies demonstrate that TA reduces cancer growth in vivo. Based on the ability of TA to mimic Lys and Arg, we hypothesized that TA may perturb multiple processes that involve Lys/Arg-rich protein sequences, and that TA may alter intracellular signaling pathways in addition to blocking extracellular Plasmin production. Indeed, TA-mediated suppression of tumor cell viability is associated with multiple biochemical actions, including inhibition of protein synthesis, reduced activating phosphorylation of STAT3 and S6K1, decreased expression of the MYC oncoprotein, and suppression of Lys acetylation. Further, TA inhibited uptake of Lys and Arg by cancer cells. These findings suggest that TA or TA analogs may serve as lead compounds and inspire the production of new classes of anticancer agents that function by mimicking Lys and Arg.

Stilbenes and Xanthones from Medicinal Plants as Potential Antitumor Agents

2020 ◽  
Vol 16 ◽  
Author(s):  
Eugenia Dumitra Teodor ◽  
Oana Ungureanu ◽  
Veronica Moroeanu ◽  
Gabriel Lucian Radu
Keyword(s):  
Medicinal Plants ◽  
Anticancer Agents ◽  
Antitumor Agents ◽  
Plant Polyphenols ◽  
Natural Substances ◽  
Abnormal Cells ◽  
Digestive Disorders ◽  
Potential Antitumor

Abstract:: There is an emerging interest for plant polyphenols as dietary ingredients, particularly in digestive disorders and/or as antitumor agents. The plant compounds or extracts continue to be an alternative to drug use, many studies being aimed to find natural substances with selective cytotoxicity on abnormal cells. Phenolic compounds as important secondary metabolites from plants are intensively studied as substitute of drugs. In this review, the recent literature data from past five years about potential anticancer/antitumor effect of some categories of phenolics such as stilbenes and xanthones extracted from medicinal plants are surveyed. The most important results concerning the effectiveness as antitumor/anticancer agents of these active compounds, as isolated compounds or as plant extracts, some bioavailability aspects and their mechanism of action in vitro and in vivo were considered.

Enhanced expression of proapoptotic and autophagic proteins involved in the cell death of glioblastoma induced by synthetic glycans

2014 ◽  
Vol 120 (6) ◽  
pp. 1298-1308 ◽  
Author(s):  
Ahmad Faried ◽  
Muhammad Zafrullah Arifin ◽  
Shogo Ishiuchi ◽  
Hiroyuki Kuwano ◽  
Shin Yazawa
Keyword(s):  
Cell Death ◽  
Mouse Model ◽  
Anticancer Agents ◽  
Anticancer Agent ◽  
Adenosine Diphosphate ◽  
Glioblastoma Cells ◽  
Enhanced Expression ◽  
Autophagic Proteins

Object Glioblastoma is the most aggressive malignant brain tumor, and overall patient survival has not been prolonged even by conventional therapies. Previously, the authors found that chemically synthesized glycans could be anticancer agents against growth of a series of cancer cells. In this study, the authors examined the effects of glycans on the growth of glioblastoma cells both in vitro and in vivo. Methods The authors investigated not only the occurrence of changes in the cell signaling molecules and expression levels of various proteins related to cell death, but also a mouse model involving the injection of glioblastoma cells following the administration of synthetic glycans. Results Synthetic glycans inhibited the growth of glioblastoma cells, induced the apoptosis of the cells with cleaved poly (adenosine diphosphate-ribose) polymerase (PARP) expression and DNA fragmentation, and also caused autophagy, as shown by the detection of autophagosome proteins and monodansylcadaverine staining. Furthermore, tumor growth in the in vivo mouse model was significantly inhibited. A dramatic induction of programmed cell death was found in glioblastoma cells after treatment with synthetic glycans. Conclusions These results suggest that synthetic glycans could be a promising novel anticancer agent for performing chemotherapy against glioblastoma.

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