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You are here: Home / Archives for 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.

Study on the expression of pepper (Capsicum annuum L.) genes and their pharmacological applications: Quercetin – Verónica Ruiz Trujillo

2 May, 2022 por Anabel Torrente Leave a Comment

This research was carried out in the Antioxidants, Free Radicals and Nitric Oxide in Biotechnology and Agri-Food Research Group (Zaidín Experimental Station, CSIC, Granada). In recent years, this group has been investigating the possible contribution that peppers can make to a better state of health, thanks to the fact that they contain compounds of pharmacological and therapeutic interest. In collaboration with the University of Malaga and the MEDINA Foundation, we conducted metabolomic and transcriptomic studies to analyse a series of metabolic pathways that lead to the synthesis of molecules with this potential capacity. These molecules are also modulated by nitric oxide (NO), a molecule whose functions in the physiology of both animal and plant cells are increasingly recognised. This Master’s Thesis takes a step further in this strategy which, together with other metabolomic data recently obtained, has allowed the group to focus its research on quercetin, one of the flavonoid compounds present in peppers, which has a number of pharmacological properties.

Keywords: Pepper; nitric oxide (NO); quercetin; flavonoid compounds.

Directed by: José Manuel Palma Martínez

 

 

Filed Under: 2020/2021, Chemical drugs. Tagged With: flavonoid compounds, nitric oxide (NO), Pepper, quercetin

Synthesis, purification and structural determination of isoquinolin-5-ol derivatives as antitumor agents – Soledad Romero Tamudo

1 May, 2022 por Anabel Torrente Leave a Comment

Cancer is a disease that begins when a cancerous cell manages to evade the main regulatory mechanisms of the cell cycle and begins to proliferate uncontrollably. It is one of the leading causes of death worldwide, so the search for new therapies is essential.
CD44 is a glycoprotein whose increased expression makes tumors more resistant to cancer treatments. Its ligand is hyaluronic acid (HA) and after binding, signaling cascades are activated that contribute to increased cell proliferation, migration and tissue invasion.
Tetrahydroisoquinoline (THIQ) inhibits binding between CD44 and HA. With this in mind, in this Master’s Thesis, we propose the synthesis of 10 isoquinolin-5-ol derivatives. We will then assess the capacity of these derivatives to act as antitumor agents by inhibiting binding between CD44 and HA.

Keywords: Cancer; CD44; Hyaluronic Acid; Tetrahydroisoquinoline; Inhibitors.

Directed by: María Dora Carrión Peregrina

Filed Under: 2020/2021, Chemical drugs. Tagged With: Cáncer, CD44, Hyaluronic Acid, Inhibitors, Tetrahydroisoquinoline

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