Coumarin Hybrids: Promising Scaffolds in the Treatment of Breast Cancer

2019 ◽  
Vol 19 (17) ◽  
pp. 1443-1458 ◽  
Author(s):  
Rohit Bhatia ◽  
Ravindra K. Rawal
Keyword(s):  
Breast Cancer ◽  
Lung Cancer ◽  
Therapeutic Agents ◽  
Toxicity Profile ◽  
Biological Targets ◽  
Organ Systems ◽  
Hybrid Molecules ◽  
Cause Of Deaths ◽  
Low Toxicity ◽  
Diverse Mode

: Breast cancer is the most common invasive cancer in women, and the second main cause of deaths in women, after lung cancer. There is continuous advancement in the development of therapeutic agents against breast cancer in recent years and it is still in progress. Development of hybrid molecules by combining different pharmacophores to obtain significant biological activity is an excellent approach. Coupling of coumarin scaffold with other distinct motifs has led to the design of newer compounds against breast cancer. These distinct pharmacophores possess a diverse mode of action as well as selectivity. It has been reported in the literature that coumarin hybrids possess significant potency against breast cancer by binding to various biological targets which are associated with breast cancer. Due to low toxicity profile on various organ systems, coumarin hybrids have nowadays attracted the keen attention of researchers to explore their therapeutic ability against breast cancer. Reported coumarin hybrids include coupling with isoxazole, thiazole, monastrol, chalcone, triazole, sulphonamide, triphenylethylene, benzimidazole, pyran, imidazole, stilbene, oestrogen, phenylsulphonylfuroxan, etc. In the present review, a description of various coumarin hybrid molecules has been presented along with their structural-activity relationships.

scholarly journals Applications of Aptamer-Bound Nanomaterials in Cancer Therapy

Biosensors ◽  
2021 ◽  
Vol 11 (9) ◽  
pp. 344
Author(s):  
Liangxi Zhu ◽  
Jingzhou Zhao ◽  
Zhukang Guo ◽  
Yuan Liu ◽  
Hui Chen ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Lung Cancer ◽  
Cancer Therapy ◽  
Cancer Treatment ◽  
Human Life ◽  
Breast Cancer Treatment ◽  
New Method ◽  
Treatment Methods ◽  
Major Disease ◽  
Low Toxicity

Cancer is still a major disease that threatens human life. Although traditional cancer treatment methods are widely used, they still have many disadvantages. Aptamers, owing to their small size, low toxicity, good specificity, and excellent biocompatibility, have been widely applied in biomedical areas. Therefore, the combination of nanomaterials with aptamers offers a new method for cancer treatment. First, we briefly introduce the situation of cancer treatment and aptamers. Then, we discuss the application of aptamers in breast cancer treatment, lung cancer treatment, and other cancer treatment methods. Finally, perspectives on challenges and future applications of aptamers in cancer therapy are discussed.

scholarly journals Design, Synthesis and Antimicrobial Evaluation of New Norfloxacin-Naphthoquinone Hybrid Molecules

Proceedings ◽  
2019 ◽  
Vol 41 (1) ◽  
pp. 9 ◽  
Author(s):  
Andrea Defant ◽  
Alessandro Vozza ◽  
Ines Mancini
Keyword(s):  
Bacterial Infections ◽  
Antimicrobial Agents ◽  
Biological Activities ◽  
Dna Gyrase ◽  
Structural Features ◽  
Therapeutic Agents ◽  
Topoisomerase Iv ◽  
Design Synthesis ◽  
Biological Targets ◽  
Hybrid Molecules

Although the wide arsenal of drugs available to treat bacterial infections, emerging drug-resistant bacterial pathogens have recently highlighted an urgent need to find new more effective and less toxic therapeutic agents. Fluoroquinolones, including norfloxacin, are antibiotics showing a concentration-dependent bactericidal capacity due to the activity inhibition of DNA-gyrase and topoisomerase IV, which are enzymes essential for bacterial DNA replication. Naphthoquinones are secondary metabolites showing different biological activities, including cytotoxic, antibacterial and antifungal effects. In particular, the efficacy of natural and synthetic 1,4-naphthoquinone derivatives is likely due to their oxidizing/reducing capability, through which they destroy cellular targets as nucleic acids. Hybrid molecules are produced combining structural features of two or more bioactive compounds, in order to obtain new therapeutic agents able, not only to reduce undesirable side effects of the parent drugs, but also to inhibit more biological targets, hopefully with a better therapeutic property than the administration of combined single-target drugs. With the aim to apply this strategy in the study of new potential antimicrobial agents, we have synthesized four hybrid molecules by the reaction of norfloxacin with suitable quinones and their activities have been evaluated against both bacteria and fungi, in comparison with synthetic precursors. The experimental data are supported by docking calculations on S. aureus DNA-gyrase, discussing the interactions involved for each hybrid molecule, in comparison with norfloxacin and the original ligand moxifloxacin.

Perbandingan CART dan Random Forest untuk Deteksi Kanker berbasis Klasifikasi Data Microarray

2020 ◽  
Vol 4 (5) ◽  
pp. 805-812
Author(s):  
Riska Chairunisa ◽  
Adiwijaya ◽  
Widi Astuti
Keyword(s):  
Breast Cancer ◽  
Lung Cancer ◽  
Ovarian Cancer ◽  
Random Forest ◽  
Classification And Regression Tree ◽  
Classification Method ◽  
Discrete Wavelet ◽  
Prostate Tumors ◽  
Cancer Data ◽  
Colon Tumors

Cancer is one of the deadliest diseases in the world with a mortality rate of 57,3% in 2018 in Asia. Therefore, early diagnosis is needed to avoid an increase in mortality caused by cancer. As machine learning develops, cancer gene data can be processed using microarrays for early detection of cancer outbreaks. But the problem that microarray has is the number of attributes that are so numerous that it is necessary to do dimensional reduction. To overcome these problems, this study used dimensions reduction Discrete Wavelet Transform (DWT) with Classification and Regression Tree (CART) and Random Forest (RF) as classification method. The purpose of using these two classification methods is to find out which classification method produces the best performance when combined with the DWT dimension reduction. This research use five microarray data, namely Colon Tumors, Breast Cancer, Lung Cancer, Prostate Tumors and Ovarian Cancer from Kent-Ridge Biomedical Dataset. The best accuracy obtained in this study for breast cancer data were 76,92% with CART-DWT, Colon Tumors 90,1% with RF-DWT, lung cancer 100% with RF-DWT, prostate tumors 95,49% with RF-DWT, and ovarian cancer 100% with RF-DWT. From these results it can be concluded that RF-DWT is better than CART-DWT.  

THE PREVALENCE OF HEPATITIS B REACTIVATION (HBV) IN CANCER PATIENTS TREATING WITH CHEMOTHERAPY

2016 ◽  
pp. 74-80
Author(s):  
Phuong Phung ◽  
Thi Thuy Nguyen
Keyword(s):  
Breast Cancer ◽  
Lung Cancer ◽  
Hepatitis B ◽  
Cancer Patients ◽  
Positive Control ◽  
High Dose ◽  
Hbv Reactivation ◽  
Endemic Region ◽  
Hepatitis B Reactivation ◽  
Cancer Breast

ackground and Objectives: Nowadays, the incidence of cancer is constantly increasing in the world as well as in Vietnam. The treatment of cancer is based on multimodality principle. Among those principal modalities, chemotherapy is widely used for different purposes such as neoadjuvant, andjuvant and palliation. However, chemotherapy can induce activation of latent infections, including hepatitis B. Vietnam is in the endemic region of hepatitis B so the reactivation of hepatitis B on cancer patients with chemotherapy has emerged a concerned problem. However, few interests were gained on this problem in the aspect of clinical setting or researching. Aims: to determine the prevalence of hepatitis B reactivation (HBV) in cancer patients treating with chemotherapy and to detect some risks factors of this situation. Subjects and methods: descriptive prospective. The study included 33 cancer patients with inactive HBV infection who are treating with chemotherapy. We define HBV reactivation by ALT > 3 ULN and HBV DNA copies > 10 positive control limit. Results: We found 6 patients with reactivated HBV, accounting for 18.18 %. Among reactivated HBV patients, age less than 60 accounts 83,33%. Rate of reactivated HBV in males was 25,00% while this rate in females was 14,28%. Rate of reactivated HBV in lymphoma, lung cancer and breast cancer was 33,33%, 25% và 22,22% respectively. Clinial manifestation of reactivated HBV includes jaundice (33,33%), fulminant hepatic failure (6%) and death (5%). The reactivated rate was higher in patients got high dose of corticoid (28,57%) vs low dose (15,38%). This rate was 29,41% in patients treated with anthracyclines which was higher than in group without anthracyclines. The reactivated rate of HBV was dramatically higher in patients treated with rituximab (75%). Conclusion: the reactivation of hepatitis B on cancer patients with chemotherapy is common. We found 6 patients with reactivated HBV of 33 subjects of the study which accounts 18.18 %. We recognized that reactivated HBV rate was higher subgroups of age < 60 years old, males, patients with lymphoma, lung cancer, breast cancer. Reactivated HBV may be more prevalent in patients with high-dose corticotherapy, anthracyclines and Rituximab. Key words: HBV reactivation, chemotherapy, cancer, hepatitis B

Recent Advances on Therapeutic Peptides for Breast Cancer Treatment

2020 ◽  
Vol 21 ◽  
Author(s):  
Samad Beheshtirouy ◽  
Farhad Mirzaei ◽  
Shirin Eyvazi ◽  
Vahideh Tarhriz
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Tumor Cells ◽  
Breast Cancer Cells ◽  
Specific Binding ◽  
High Specificity ◽  
The Novel ◽  
Anti Cancer ◽  
Therapeutic Peptides ◽  
Low Toxicity

: Breast cancer is a heterogeneous malignancy which is the second cause of mortality among women in the world. Increasing the resistance to anti-cancer drugs in breast cancer cells persuades researchers to search the novel therapies approaches for the treatment of the malignancy. Among the novel methods, therapeutic peptides which target and disrupt tumor cells have been of great interest. Therapeutic peptides are short amino acids monomer chains with high specificity to bind and modulate a protein interaction of interest. Several advantages of peptides such as specific binding on tumor cells surface, low molecular weight and low toxicity on normal cells make the peptides as an appealing therapeutic agents against solid tumors, particularly breast cancer. Also, National Institutes of Health (NIH) describes therapeutic peptides as suitable candidate for the treatment of drug-resistant breast cancer. In this review, we attempt to review the different therapeutic peptides against breast cancer cells which can be used in treatment and diagnosis of the malignancy. Meanwhile, we presented an overview of peptide vaccines which have been developed for the treatment of breast cancer.

Cancer as a Scottish Problem

1968 ◽  
Vol 13 (10) ◽  
pp. 338-348
Author(s):  
A. J. Haddow
Keyword(s):  
Breast Cancer ◽  
Lung Cancer ◽  
Cause Of Death ◽  
Cancer Mortality ◽  
Time Lag ◽  
Age Distribution ◽  
Lung Cancer Mortality ◽  
Cervix Uteri ◽  
Hospital Treatment ◽  
Cancer Of The Lung

Cancer, responsible for about 1 death in 5 in Scotland, cost over £1 per head of population in 1965 and led to bed occupation of almost 2,000 bed years. Time lag (symptoms-doctor-hospital-treatment) is usuallv small. Age distribution is as in other European countries. Excluding accidents, cancer is the second most important cause of death in children. In relation to other countries Scotland's position is very poor and the lung cancer mortality in both sexes is the highest known. Lung cancer is the most important in males, breast cancer in females. Alimentary cancers come second in both sexes. In this century alimentary cancers increased till the thirties or forties and then declined. Cancers of pancreas, cervix uteri, ovary, prostate, kidney and bladder, together with leukaemia, have all increased. Cancer of the lung has increased elevenfold in women and fiftyfold in men. It now accounts for 9 to 12 per cent of all male deaths in cities and large towns

Antiestrogen use in breast cancer patients reduces the risk of subsequent lung cancer: A population-based study

2017 ◽  
Vol 48 ◽  
pp. 22-28 ◽  
Author(s):  
Sung-Chao Chu ◽  
Chia-Jung Hsieh ◽  
Tso-Fu Wang ◽  
Mun-Kun Hong ◽  
Tang-Yuan Chu
Keyword(s):  
Breast Cancer ◽  
Lung Cancer ◽  
Cancer Patients ◽  
Population Based ◽  
Breast Cancer Patients ◽  
Population Based Study

scholarly journals Biosynthesis of Nature-Inspired Unnatural Cannabinoids

Molecules ◽  
2021 ◽  
Vol 26 (10) ◽  
pp. 2914
Author(s):  
Kevin J. H. Lim ◽  
Yan Ping Lim ◽  
Yossa D. Hartono ◽  
Maybelle K. Go ◽  
Hao Fan ◽  
...  
Keyword(s):  
Synthetic Biology ◽  
Cannabis Sativa ◽  
Genetic Manipulation ◽  
Therapeutic Agents ◽  
Orphan Receptors ◽  
Complex Chemical ◽  
Biological Targets ◽  
Chemical Structures ◽  
Commercial Use ◽  
Wide Range

Natural products make up a large proportion of medicine available today. Cannabinoids from the plant Cannabis sativa is one unique class of meroterpenoids that have shown a wide range of bioactivities and recently seen significant developments in their status as therapeutic agents for various indications. Their complex chemical structures make it difficult to chemically synthesize them in efficient yields. Synthetic biology has presented a solution to this through metabolic engineering in heterologous hosts. Through genetic manipulation, rare phytocannabinoids that are produced in low yields in the plant can now be synthesized in larger quantities for therapeutic and commercial use. Additionally, an exciting avenue of exploring new chemical spaces is made available as novel derivatized compounds can be produced and investigated for their bioactivities. In this review, we summarized the biosynthetic pathways of phytocannabinoids and synthetic biology efforts in producing them in heterologous hosts. Detailed mechanistic insights are discussed in each part of the pathway in order to explore strategies for creating novel cannabinoids. Lastly, we discussed studies conducted on biological targets such as CB1, CB2 and orphan receptors along with their affinities to these cannabinoid ligands with a view to inform upstream diversification efforts.

Sign in / Sign up

Export Citation Format

Share Document