Recent Developments in Anticancer Activity of Compounds Containing the Thioether Group

2020 ◽  
Vol 20 ◽  
Author(s):  
Muhammad İ. Han ◽  
Şükriye G. Küçükgüzel
Keyword(s):  
Anticancer Activity ◽  
Anticancer Agents ◽  
Research Field ◽  
Cancer Development ◽  
Anticancer Activities ◽  
Cancer Disease ◽  
New Class ◽  
Research Activities ◽  
Recent Developments ◽  
Patent Literature

Background: Spreading rapidly in recent years, cancer has become the cause of one of the highest mortality rates after cardiovascular diseases. With more attention being directed to cancer, anticancer research has become an important research field. In spite of enormous research activities in this area, the reason for cancer development is still not clearly understood. Scientists are now working on the biology of cancer, especially on the root of the cause for cancer development. The aim is to treat the cancer disease, and thus cure the patients. Continuing efforts on the development of novel molecules as potential anticancer agents is essential for this purpose. Objective: The main aim of this review was to present a survey on the medicinal chemistry of thioethers and to provide practical data on their cytotoxicities against various cancer cell lines. Methods: Research articles published between 2001-2019 were consulted in the preparation of this review article though patent literature was not included here. Results: Compounds containing thioether functionality were proven to have anticancer activities. Indeed, thioether functionality was found to be a must in some cases to show anticancer activity. Conclusion: Thioether containing molecules may emerge as new class of potent and effective anticancer agents in the near future.

Thioethers: An Overview

2021 ◽  
Vol 22 ◽  
Author(s):  
M İhsan Han ◽  
Ş. Güniz Küçükgüzel
Keyword(s):  
Heterocyclic Compounds ◽  
Mortality Rates ◽  
Review Article ◽  
Cancer Development ◽  
Cancer Disease ◽  
Root Cause ◽  
New Class ◽  
Research Activities ◽  
Anti Cancer ◽  
Patent Literature

: Spreading rapidly in recent years, cancer has become the cause of one of the highest mortality rates after cardiovascular diseases. The reason for cancer development is still not clearly understood despite enormous research activities in this area. Scientists are now working on the biology of cancer, especially on the root cause of cancer development. The aim is to treat the cancer disease, and thus cure the patients. The continuing efforts on the development of novel molecules as potential anti-cancer agents are essential for this purpose. The main aim of this review was to present a survey on the medicinal chemistry of thioethers and to provide practical data on their cytotoxicities against various cancer cell lines. The research articles published between 2001-2020 were consulted in the preparation of this review article, though patent literature was not included here. The thioether-containing heterocyclic compounds may emerge as a new class of potent and effective anti-cancer agents soon.

scholarly journals NBM-HD-1: A Novel Histone Deacetylase Inhibitor with Anticancer Activity

2012 ◽  
Vol 2012 ◽  
pp. 1-11 ◽  
Author(s):  
Wei-Jan Huang ◽  
Yu-Chih Liang ◽  
Shuang-En Chuang ◽  
Li-Ling Chi ◽  
Chi-Yun Lee ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cancer Cells ◽  
Anticancer Agents ◽  
Xenograft Model ◽  
Cyclin B1 ◽  
Dependent Manner ◽  
Cell Cycle Regulators ◽  
Anticancer Activities ◽  
Gene Expressions

HDAC inhibitors (HDACis) have been developed as promising anticancer agents in recent years. In this study, we synthesized and characterized a novel HDACi, termed NBM-HD-1. This agent was derived from the semisynthesis of propolin G, isolated from Taiwanese green propolis (TGP), and was shown to be a potent suppressor of tumor cell growth in human breast cancer cells (MCF-7 and MDA-MB-231) and rat glioma cells (C6), with an IC50ranging from 8.5 to 10.3 μM. Western blot demonstrated that levels of p21(Waf1/Cip1), gelsolin, Ac-histone 4, and Ac-tubulin markedly increased after treatment of cancer cells with NBM-HD-1. After NBM-HD-1 treatment for 1–4 h, p-PTEN and p-AKT levels were markedly decreased. Furthermore, we also found the anticancer activities of NBM-HD-1 in regulating cell cycle regulators. Treatment with NBM-HD-1,p21(Waf1/Cip1)gene expression had markedly increased whilecyclin B1andD1gene expressions had markedly decreased. On the other hand, we found that NBM-HD-1 increased the expressions of tumor-suppressor genep53in a dose-dependent manner. Finally, we showed that NBM-HD-1 exhibited potent antitumor activity in a xenograft model. In conclusion, this study demonstrated that this compound, NBM-HD-1, is a novel and potent HDACi with anticancer activityin vitroandin vivo.

Design, Synthesis, Anticancer Evaluation, and Molecular Docking Studies of Novel Benzoxazole Linked 1,3,4-Oxadiazoles

2021 ◽  
Vol 21 ◽  
Author(s):  
Sushmitha Bujji ◽  
Praveen Kumar E ◽  
Sree Kanth Sivan ◽  
Manjunatha DH ◽  
Subhashini N.J.P.
Keyword(s):  
Molecular Docking ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Research Work ◽  
Docking Simulation ◽  
Research Field ◽  
Spectroscopic Techniques ◽  
Cancer Disease ◽  
Amide Derivatives

Background: Cancer disease is making a serious concern globally. Global cancer occurrence is steadily increasing every year. There is always a persistent need to develop new anticancer drugs with reduced side effects or act synergistically with the existing chemotherapeutics. Objective: Benzoxazoles are fused bicyclic nitrogen and oxygen-containing heterocyclic compounds and are considered biologically privileged scaffolds. We designed a synthetic route to link the benzoxazoles with oxadiazoles resulting in a better pharmacophore for anticancer activity. Methods: A series of novel amide derivatives of benzoxazole linked 1,3,4-oxadiazoles (10a-j) were synthesized and characterized by 1H NMR, 13C NMR, and mass spectroscopic techniques. The biological properties of the compounds were screened in vitro against four different tumor cell lines. Results: The results suggest that the compound 10b having 3,4,5-trimethoxy substitution on the phenyl ring exhibited potent anticancer activity in three cell lines (A549 = 0.13 ± 0.014 µM, MCF-7 = 0.10 ± 0.013 µM and HT-29 = 0.22 ± 0.017 µM). Notably, among the synthesized derivatives, compounds 10b, 10c, 10f, 10g, and 10i exhibited potent anticancer activity than the control IC50 in the range of 0.11 ± 0.02 to 0.93 ± 0.034 µM. Molecular docking simulation results showed compounds were stabilized by hydrogen bond and π-π interactions with the protein. Conclusion: The molecules showed comparable binding affinities with standard Combretastatin-A4. The present research work is preliminary and needs further studies to take the synthesized compounds to the next level in the cancer research field.

scholarly journals DNA-Binding and Topoisomerase-I-Suppressing Activities of Novel Vanadium Compound Van-7

2012 ◽  
Vol 2012 ◽  
pp. 1-9 ◽  
Author(s):  
Xiao-mei Mo ◽  
Zhan-fang Chen ◽  
Xin Qi ◽  
Yan-tuan Li ◽  
Jing Li
Keyword(s):  
Dna Binding ◽  
Anticancer Agents ◽  
Topoisomerase I ◽  
A549 Cells ◽  
Anticancer Activities ◽  
Vanadium Compound ◽  
New Class ◽  
M Phase ◽  
Low Toxicity ◽  
Topo Ii

Vanadium compounds were studied during recent years to be considered as a representative of a new class of nonplatinum metal anticancer agents in combination to its low toxicity. Here, we found a vanadium compound Van-7 as an inhibitor of Topo I other than Topo II using topoisomerase-mediated supercoiled DNA relaxation assay. Agarose gel electrophoresis and comet assay showed that Van-7 treatment did not produce cleavable complexes like HCPT, thereby suggesting that Topo I inhibition occurred upstream of the relegation step. Further studies revealed that Van-7 inhibited Topo I DNA binding involved in its intercalating DNA. Van-7 did not affect the catalytic activity of DNase I even up to100 μM. Van-7 significantly suppressed the growth of cancer cell lines with IC50at nanomolar concentrations and arrested cell cycle of A549 cells at G2/M phase. All these results indicate that Van-7 is a potential selective Topo I inhibitor with anticancer activities as a kind of Topo I suppressor, not Topo I poison.

Synthesis, characterization, optical and electrochemical properties and antifungal and anticancer activities of ferrocenyl conjugated novel dendrimers

2017 ◽  
Vol 41 (4) ◽  
pp. 1714-1722 ◽  
Author(s):  
Velautham Saravanan ◽  
Ayyavoo Kannan ◽  
Perumal Rajakumar
Keyword(s):  
Antifungal Activity ◽  
Electrochemical Properties ◽  
Anticancer Activity ◽  
Click Chemistry ◽  
Fungal Pathogens ◽  
Anticancer Activities ◽  
New Class ◽  
Mcf 7

A new class of triazoloferrocenyl conjugates was prepared by copper(i) catalyzed click chemistry, which shows good antifungal activity against fungal pathogens, and also shows excellent anticancer activity against MCF-7 cells.

scholarly journals Synthesis, Anticancer and Molecular Docking Studies of N-(1H-benzimidazol-2-yl-carbamothioyl)benzamide Analogues

2020 ◽  
pp. 204-212 ◽  
Author(s):  
Priyanka P. Rode ◽  
Akshay R. Yadav ◽  
Ankita V. Chitruk ◽  
Shrinivas K. Mohite ◽  
Chandrakant S. Magdum
Keyword(s):  
Molecular Docking ◽  
Anticancer Activity ◽  
Anticancer Agents ◽  
Treatment Options ◽  
Specific Treatment ◽  
Docking Studies ◽  
Cancer Resistance ◽  
Cancer Disease ◽  
Molecular Docking Studies

A series of novel N-(1H-benzimidazole-2-yl-carbamothioyl)benzamide derivatives were synthesized under microwave irradiation and evaluated for anticancer activity. The synthesized compounds were characterized by IR, 1H-NMR, and mass spectral data. Complexity associated with cancer disease and prevalence of diversified cell populations vindicates highly specific treatment options for treatment of cancer. Resistance to these anticancer agents has posed a great hindrance in successful treatment of cancer. Pondering this ongoing situation, it was speculated to develop novel compounds targeting cancer. All the newly synthesized compounds 3a-f were further evaluated for anticancer activity against MCF-7 cell lines using MTT assay. Molecular docking studies were performed using VLife MDS 4.3 software. The compounds 3c exhibited good docking scores of -60.37. The anticancer and docking results highlight the fact that the synthesized compounds 3c could be considered as possible hit as therapeutic agents. A significant correlation was observed between the in silico and the in vitro studies.

Design, Synthesis, SAR Study, Antimicrobial and Anticancer Evaluation of Novel 2-Mercaptobenzimidazole Azomethine Derivatives

2020 ◽  
Vol 20 (15) ◽  
pp. 1559-1571 ◽  
Author(s):  
Sumit Tahlan ◽  
Balasubramanian Narasimhan ◽  
Siong Meng Lim ◽  
Kalavathy Ramasamy ◽  
Vasudevan Mani ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Anticancer Agents ◽  
Benzimidazole Derivatives ◽  
Dilution Method ◽  
Anticancer Activities ◽  
Design Synthesis ◽  
Standard Drug ◽  
Wide Range ◽  
Sar Study

Background: Various analogues of benzimidazole are found to be biologically and therapeutically potent against several ailments. Benzimidazole when attached with heterocyclic rings has shown wide range of potential activities. So, from the above provided facts, we altered benzimidazole derivatives so that more potent antagonists could be developed. In the search for a new category of antimicrobial and anticancer agents, novel azomethine of 2-mercaptobenzimidazole derived from 3-(2- (1H-benzo[d]imidazol-2-ylthio)acetamido)benzohydrazide were synthesized. Results and Discussion: The synthesized analogues were characterized by FT-IR, 1H/13C-NMR and MS studies as well C, H, N analysis. All synthesized compounds were evaluated for in vitro antibacterial activity against Gram-positive (B. subtilis), Gram-negative (E. coli, P. aeruginosa, K. pneumoniae and S. typhi) strains and in vitro antifungal activity against C. albicans and A. niger strains by serial dilution method, the minimum inhibitory concentration (MIC) described in μM/ml. The in vitro anticancer activity of synthesized compounds was determined against human colorectal carcinoma cell line (HCT- 116) using 5-fluorouracil as standard drug. Conclusion: In general, most of the synthesized derivatives exhibited significant antimicrobial and anticancer activities. Compounds 8, 10, 15, 16, 17, 20 and 22 showed significant antimicrobial activity towards tested bacterial and fungal strains and compound 26 exhibited significant anticancer activity.

Breaking the Barrier of Cancer through Papaya Extract and their Formulation

2019 ◽  
Vol 19 (13) ◽  
pp. 1577-1587
Author(s):  
Sumana Saha ◽  
Tapan Kumar Giri
Keyword(s):  
Literature Search ◽  
Carica Papaya ◽  
Research Field ◽  
Anticancer Activities ◽  
Carcinogenic Potential ◽  
Recent Developments ◽  
Costs Of Treatment ◽  
Animal Resources ◽  
Important Branch ◽  
Different Parts

Background: In the last decade, many new avenues of cancer treatment have opened up but the costs of treatment have sky-rocketed too. Hence, screening of indigenously available plant and animal resources for anti-carcinogenic potential is an important branch of anticancer research. The effort has been made through this comprehensive review to highlight the recent developments of anticancer therapies using different parts of papaya plant extract. Methods: In search of the naturally existing animals and plants for anticarcinogenic potential, papaya plant has been exploited by the scientist working in this research field. A widespread literature search was performed for writing this review. Results: Different constituents of Carica papaya responsible for anticancer activities have been discussed. Papaya extract for the treatment of breast, liver, blood, pancreas, skin, prostate, and colon cancer have also been reported. Finally, the various formulation approach using Carica papaya extract have been highlighted. Conclusion: The information provided in this review might be useful for researchers in designing of novel formulation of Carica papaya extract for the treatment of cancer.

scholarly journals Copper(II) complexes of Schiff base ligands as promising anticancer agents

2016 ◽  
Author(s):  
Elżbieta Hejchman ◽  
Barbara Sowirka ◽  
Magdalena Tomczyk ◽  
Dorota Maciejewska
Keyword(s):  
Schiff Base ◽  
Anticancer Activity ◽  
Schiff Bases ◽  
Anticancer Agents ◽  
Copper Complexes ◽  
World Health ◽  
Anticancer Activities ◽  
Schiff Base Ligands ◽  
Drug Induced

Based on World Health Organization (WHO) report, it was estimated that one in five people before age 75 will suffer from cancer during their lifetime, and more than 13 million cancers death will happen in 2030. Chemotherapy is a basic approach for the treatment of cancer diseases. However, because of drug resistance and considerable side effects drug-induced toxicity, the discovery of new metal analogs with promising activity and high therapeutic index is an urgent need. The fundamental role of copper and the recognition of its complexes as important bioactive compounds in vitro and in vivo aroused an ever-increasing interest in these agents as potential drugs for therapeutic intervention in various diseases. Schiff bases are a critical class of compounds in medical chemistry that have demonstrated significant chemotherapeutic and antibacterial application. Schiff base Cu(II) complexes revealed great potential for antiproliferative, antibacterial, and gastroprotective activity. Coumarins are a wide class of natural and synthetic compounds that showed diverse pharmacological activities including anticancer activity. Among the wide variety of coumarins, 7-hydroxycoumarin derivatives have been shown to possess desirable antiproliferative activities. In particular, their antibacterial, antifungal and anticancer activities make the compounds attractive for further derivatization and screening as novel therapeutic agents. Taking these compounds as lead, we have designed and synthesized a series of new copper(II) complexes with coumarin-derived Schiff base ligands. Two series of Schiff bases were prepared by condensation of 8-formyl-7-hydroxy-4-methylcoumarin and 8-acetyl-7-hydroxy-4-methylcoumarin with p-substituted aniline derivatives. These compounds were used as ligands in the synthesis of copper(II) complexes. The obtained Schiff bases as well as copper complexes are mostly novel molecules. Only the products of condensation 8-formyl-7-hydroxy-4-methylcoumarin with p-toluidine and 8-acetyl-7-hydroxy-4-methylcoumarin with p-toluidine and its copper(II) complex were synthesized, but the anticancer activity of these compounds was not determined. The assay of their cytotoxic activity is in progress. Preliminary, we have identified two copper(II) coordination compounds of 7-hydroxy-8-[1-(4-methoxyphenyl imino)ethyl]-4-methyl-2H-chromen-2-one and 7-hydroxy-8-[1-(4-hydroxyphenyloimino)ethyl]-4-methyl-2H- chromen-2-one having dose-dependent antiproliferative activity on HeLa cancer cell line. Additionally, the Schiff bases – derivatives of substituted salicylaldehydes and 2-hydroxyacetophenones condensed with appropriate anilines were prepared. Such compounds have been reported in scientific papers, their copper complexes have not been assayed yet, and may serve as an useful tool in QSAR investigation.

scholarly journals Copper(II) complexes of Schiff base ligands as promising anticancer agents

2016 ◽  
Author(s):  
Elżbieta Hejchman ◽  
Barbara Sowirka ◽  
Magdalena Tomczyk ◽  
Dorota Maciejewska
Keyword(s):  
Schiff Base ◽  
Anticancer Activity ◽  
Schiff Bases ◽  
Anticancer Agents ◽  
Copper Complexes ◽  
World Health ◽  
Anticancer Activities ◽  
Schiff Base Ligands ◽  
Drug Induced

Based on World Health Organization (WHO) report, it was estimated that one in five people before age 75 will suffer from cancer during their lifetime, and more than 13 million cancers death will happen in 2030. Chemotherapy is a basic approach for the treatment of cancer diseases. However, because of drug resistance and considerable side effects drug-induced toxicity, the discovery of new metal analogs with promising activity and high therapeutic index is an urgent need. The fundamental role of copper and the recognition of its complexes as important bioactive compounds in vitro and in vivo aroused an ever-increasing interest in these agents as potential drugs for therapeutic intervention in various diseases. Schiff bases are a critical class of compounds in medical chemistry that have demonstrated significant chemotherapeutic and antibacterial application. Schiff base Cu(II) complexes revealed great potential for antiproliferative, antibacterial, and gastroprotective activity. Coumarins are a wide class of natural and synthetic compounds that showed diverse pharmacological activities including anticancer activity. Among the wide variety of coumarins, 7-hydroxycoumarin derivatives have been shown to possess desirable antiproliferative activities. In particular, their antibacterial, antifungal and anticancer activities make the compounds attractive for further derivatization and screening as novel therapeutic agents. Taking these compounds as lead, we have designed and synthesized a series of new copper(II) complexes with coumarin-derived Schiff base ligands. Two series of Schiff bases were prepared by condensation of 8-formyl-7-hydroxy-4-methylcoumarin and 8-acetyl-7-hydroxy-4-methylcoumarin with p-substituted aniline derivatives. These compounds were used as ligands in the synthesis of copper(II) complexes. The obtained Schiff bases as well as copper complexes are mostly novel molecules. Only the products of condensation 8-formyl-7-hydroxy-4-methylcoumarin with p-toluidine and 8-acetyl-7-hydroxy-4-methylcoumarin with p-toluidine and its copper(II) complex were synthesized, but the anticancer activity of these compounds was not determined. The assay of their cytotoxic activity is in progress. Preliminary, we have identified two copper(II) coordination compounds of 7-hydroxy-8-[1-(4-methoxyphenyl imino)ethyl]-4-methyl-2H-chromen-2-one and 7-hydroxy-8-[1-(4-hydroxyphenyloimino)ethyl]-4-methyl-2H- chromen-2-one having dose-dependent antiproliferative activity on HeLa cancer cell line. Additionally, the Schiff bases – derivatives of substituted salicylaldehydes and 2-hydroxyacetophenones condensed with appropriate anilines were prepared. Such compounds have been reported in scientific papers, their copper complexes have not been assayed yet, and may serve as an useful tool in QSAR investigation.

Sign in / Sign up

Export Citation Format

Share Document