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You are here: Home / Archives for Chemical drugs.

New combined drugs: antibiotic + anti-inflammatory – Ana Cruz Muñoz

15 May, 2023 por Anabel Torrente Leave a Comment

Most drugs on the market have properties that could be improved, of which solubility is the most common. Solubility is important because it affects absorption, that is, the amount of drug that enters the body. Low absorption means that the drug cannot reach its destination and does not have sufficient effect. If this happens, the dose must be increased, so raising not only the costs of the treatment but also the side effects. Various different techniques can be applied to solve this problem, one of which involves binding the drugs to other molecules that improve the solubility of the drug without affecting its action. Sometimes, these molecules can be other drugs, so that in addition to improving the properties, we can create a “multi-drug” that is very useful in combination therapies. 

The aim of the study is to combine two drugs: an antibiotic and a non-steroidal anti-inflammatory drug (NSAID), such as flurbiprofen. To this end, we carried out mechanochemical syntheses, such as grinding, which enable the formation of bonds between the two drugs, giving rise to salts. Once we had obtained the drug-drug salts, we then conducted characterization, stability and solubility studies on them to assess their viability. 

Keywords: antibiotic, anti-inflammatory, solubility, absorption, multidrug. 

Directed by: Alicia Domínguez Martín 

Filed Under: 2022/2023, Chemical drugs.

Design, synthesis and biological evaluation of new compounds for treating cancer – Iria Alonso Alves

15 May, 2023 por Anabel Torrente Leave a Comment

Cancer is still one of the leading causes of death worldwide, and despite the increased development of chemotherapeutic drugs, they still have many limitations, making the search for new antitumor drugs essential.  

Cancer cells are characterized by their uncontrolled proliferation and growth, which is why, as expected, they suffer alterations in their metabolism. These cells generally consume a large amount of glucose, amino acids and lipids. Lipids can act as a source of energy and are common components of cell membranes. The various alterations in lipid metabolism include the overexpression of a molecule known as choline kinase. Choline kinase is an enzyme, which will be one of the targets of the anticancer compounds that we will be developing in this research. 

We hope that these compounds will be capable of inhibiting both the growth of cancer cells (antiproliferative activity) and cell division processes (antimitotic activity). In this way, the synthesized molecules would act simultaneously against different biological targets, and could form the basis for more effective cancer treatment. 

Keywords: cancer, choline kinase, antiproliferative activity, antimitotic activity 

Directed by: Luisa Carlota López Cara 

Filed Under: 2022/2023, Chemical drugs.

Design and study of new drugs with possible antitumor activity – Noelia Ruiz Cuevas

8 May, 2022 por Anabel Torrente Leave a Comment

 

CD44 is a membrane receptor found in various types of cells in our body. This receptor binds mainly to hyaluronic acid (HA). The interaction of HA with CD44 induces changes that trigger rapid growth (proliferation) of cancer cells. Inhibition of this interaction could therefore interrupt tumour progression.
There is a specific place (small pocket) in the structure of CD44 in which small molecules could be introduced that would act as inhibitors of tumour activity. The first structures to show inhibitory activity when interacting with this pocket were molecules known as tetrahydroisoquinoline derivatives. However, it is difficult to assess the capacity of these molecules as possible antitumor agents due to their poor solubility. The main objective of this research is therefore to synthesize a series of isoquinoline salts that have good solubility in water, so facilitating the biological evaluation of these molecules.
These molecules are obtained via the reaction of isoquinoline with a chemical compound, the 3,4,5-trimethoxybenzyl group, and the introduction of different substituents in its structure, specifically in a structure known as an aromatic ring. These substitutions enable us to study the structure-activity relationship and the effect on the binding of the molecules to the aforementioned pocket in CD44.

Keywords: cancer; inhibitors; hyaluronic acid; CD44; isoquinoline.

Directed by: Olga Cruz López

Filed Under: 2021/2022, Chemical drugs. Tagged With: Cáncer, CD44, Hyaluronic Acid, Inhibitors, isoquinoline.

Designing new drugs for the treatment of cancer – Laura Erviti Marticorena

7 May, 2022 por Anabel Torrente Leave a Comment

 

CD44 is a protein that is found on the surface of human cells. It interacts with another protein, hyaluronic acid (HA), causing normal cells to become tumour cells, so enabling tumour development, metastasis and resistance to drug treatment. HA-CD44 interaction is therefore an interesting pharmacological target in cancer therapy.
The main objective of this project is the design, synthesis, and biological evaluation of inhibitors of HA-CD44 interaction, known as derivatives of 1,2,3,4-tetrahydroisoquinoline (THIQ). These molecules act as antitumor agents because they bind to CD44 in a place close to where HA binds, thus inhibiting HA-CD44 interaction. To this end, in this project we study the influence of small variations in the structure of 1,2,3,4-tetrahydroisoquinoline on the inhibition of the HA-CD44 interaction.

Keywords: cancer; inhibitors; hyaluronic acid; CD44, isoquinoline.

Directed by: Ana Conejo García

Filed Under: 2021/2022, Chemical drugs. Tagged With: Cáncer, CD44, Hyaluronic Acid, Inhibitors, isoquinoline.

5-quinolinol derivatives as potential antitumor agents. – Alba Domínguez Encinas

7 May, 2022 por Anabel Torrente Leave a Comment

 

Nowadays, cancer is the second greatest cause of death worldwide, with an estimated 10 million deaths in 2020. Although many chemotherapy drugs are used in clinical practice, we still face two challenges: (a) some patients acquire resistance to anti-tumour drugs after long periods of treatment; (b) these drugs can have toxic effects on healthy cells and tissues. The development of new anti-cancer drugs is therefore essential.
Research shows that hyaluronic acid (HA) can encourage the growth and development of tumours as it interacts with the CD44 protein located on the surface of tumour cells. It has also been noted that compounds known as isoquinoline derivatives can inhibit tumour cell growth (antiproliferative activity) by inhibiting HA-CD44 binding.
In this master’s thesis we aim to synthesize a series of 5-quinolinol derivatives (isoquinoline derivatives) to evaluate their antiproliferative activity and the process by which they inhibit HA-CD44 binding.

Keywords: cancer; CD44; hyaluronic acid; quinolinoline; inhibitors

Directed by: Mª Dora Carrión Peregrina

Filed Under: 2021/2022, Chemical drugs.

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