MALARIA Synthesis of Hybrid Molecules and Inhibitors of Falcipain for Use as Therapeutic Agents in Treatment of Malaria

: 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.

Download Full-text

Bile Acid Conjugates with Anticancer Activity: Most Recent Research

Molecules ◽

10.3390/molecules26010025 ◽

2020 ◽

Vol 26 (1) ◽

pp. 25

Author(s):

Maria Luisa Navacchia ◽

Elena Marchesi ◽

Daniela Perrone

Keyword(s):

Bile Acid ◽

Cancer Therapy ◽

Anticancer Activity ◽

Bile Acids ◽

Treatment Modality ◽

Biological Properties ◽

Therapeutic Agents ◽

Bioactive Molecules ◽

Hybrid Functional ◽

Hybrid Molecules

The advantages of a treatment modality that combines two or more therapeutic agents in cancer therapy encourages the study of hybrid functional compounds for pharmacological applications. In light of this, we reviewed recent works on hybrid molecules based on bile acids. Due to their biological properties, as well as their different chemical/biochemical reactive moieties, bile acids can be considered very interesting starting molecules for conjugation with natural or synthetic bioactive molecules.

Download Full-text

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

Proceedings ◽

10.3390/ecsoc-23-06480 ◽

2019 ◽

Vol 41 (1) ◽

pp. 9 ◽

Cited By ~ 1

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.

Download Full-text

Water-soluble amphiphilic ruthenium(ii) polypyridyl complexes as potential light-activated therapeutic agents

Chemical Communications ◽

10.1039/d0cc04397d ◽

2020 ◽

Vol 56 (65) ◽

pp. 9332-9335

Author(s):

Sandra Estalayo-Adrián ◽

Salvador Blasco ◽

Sandra A. Bright ◽

Gavin J. McManus ◽

Guillermo Orellana ◽

...

Keyword(s):

Cervical Cancer ◽

Cancer Cells ◽

Cellular Uptake ◽

Therapeutic Agents ◽

Water Soluble ◽

Polypyridyl Complexes ◽

Cervical Cancer Cells

Two new water-soluble amphiphilic Ru(ii) polypyridyl complexes were synthesised and their photophysical and photobiological properties evaluated; both complexes showed a rapid cellular uptake and phototoxicity against HeLa cervical cancer cells.

Download Full-text

Flavonoids in adipose tissue inflammation and atherosclerosis: one arrow, two targets

Clinical Science ◽

10.1042/cs20200356 ◽

2020 ◽

Vol 134 (12) ◽

pp. 1403-1432 ◽

Cited By ~ 2

Author(s):

Manal Muin Fardoun ◽

Dina Maaliki ◽

Nabil Halabi ◽

Rabah Iratni ◽

Alessandra Bitto ◽

...

Keyword(s):

Adipose Tissue ◽

Fruits And Vegetables ◽

Metabolic Diseases ◽

Therapeutic Agents ◽

Adipose Tissue Inflammation ◽

Cellular Mechanisms ◽

Tissue Inflammation ◽

Cholesterol Levels ◽

Naturally Occurring ◽

Pro Inflammatory Cytokines

Abstract Flavonoids are polyphenolic compounds naturally occurring in fruits and vegetables, in addition to beverages such as tea and coffee. Flavonoids are emerging as potent therapeutic agents for cardiovascular as well as metabolic diseases. Several studies corroborated an inverse relationship between flavonoid consumption and cardiovascular disease (CVD) or adipose tissue inflammation (ATI). Flavonoids exert their anti-atherogenic effects by increasing nitric oxide (NO), reducing reactive oxygen species (ROS), and decreasing pro-inflammatory cytokines. In addition, flavonoids alleviate ATI by decreasing triglyceride and cholesterol levels, as well as by attenuating inflammatory mediators. Furthermore, flavonoids inhibit synthesis of fatty acids and promote their oxidation. In this review, we discuss the effect of the main classes of flavonoids, namely flavones, flavonols, flavanols, flavanones, anthocyanins, and isoflavones, on atherosclerosis and ATI. In addition, we dissect the underlying molecular and cellular mechanisms of action for these flavonoids. We conclude by supporting the potential benefit for flavonoids in the management or treatment of CVD; yet, we call for more robust clinical studies for safety and pharmacokinetic values.

Download Full-text

Antithrombotic Therapy for DVT/PE

Hämostaseologie ◽

10.1055/s-0038-1659983 ◽

1997 ◽

Vol 17 (03) ◽

pp. 161-162

Author(s):

Thomas Hyers

Keyword(s):

Molecular Weight ◽

Low Molecular Weight Heparin ◽

Oral Anticoagulants ◽

Cost Effective ◽

Therapeutic Agents ◽

Great Promise ◽

Term Therapy ◽

Low Molecular Weight ◽

Long Term Therapy

SummaryProblems with unfractionated heparin as an antithrombotic have led to the development of new therapeutic agents. Of these, low molecular weight heparin shows great promise and has led to out-patient therapy of DVT/PE in selected patients. Oral anticoagulants remain the choice for long-term therapy. More cost-effective ways to give oral anticoagulants are needed.

Download Full-text

Imaging of central cannabinoid CB1 receptors, a potential target for therapeutic agents in movement disorders

Aktuelle Neurologie ◽

10.1055/s-2005-916290 ◽

2005 ◽

Vol 32 (06) ◽

Author(s):

G Berding ◽

U Schneider ◽

P Gielow ◽

R Buchert ◽

WH Knapp ◽

...

Keyword(s):

Movement Disorders ◽

Therapeutic Agents ◽

Cb1 Receptors ◽

Potential Target

Download Full-text

Pharmaconutrition: pharmacological approach to nutrition therapy

Orvosi Hetilap ◽

10.1556/oh.2014.29974 ◽

2014 ◽

Vol 155 (51) ◽

pp. 2021-2027

Author(s):

István Télessy

Keyword(s):

Fatty Acids ◽

Nutritional Support ◽

Pharmacological Action ◽

Nutrition Therapy ◽

Therapeutic Agents ◽

Therapeutic Action ◽

Treatment Results ◽

Research Activity ◽

Therapeutic Modalities ◽

The Everyday

Reviewing the literature of nutrition therapy one can conclude that during the last decade the pharmacological action of several nutrients has been demonstrated. However, research activity is still at the beginning and it could be verified in a restricted number of nutrients only that in which conditions (illnesses), dose and duration we can expect therapeutic effect in addition to nutrition. The examples of glutamine, arginine, taurine, leucine, ω-3 fatty acids, however, support the possibility that complex reactions and treatment results observed in certain patients are not purely due to nutritional support but the consequence of additional pharmacological action as well. Evaluation of results of therapeutic intervention is especially difficult because in the everyday practice physicians try to use several therapeutic modalities that can be beneficial for the patient. Therefore, retrospective separation of beneficial components of the therapeutic agents is almost impossible. Only well designed, randomized and multicentric studies can verify specific therapeutic action of certain ingredients ie. nutrients. Orv. Hetil., 2014, 155(51), 2021–2027.

Download Full-text