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Development and dermatological screening of a hemisynthetic library

(i) development of a high molecular diversity library, made by hemi synthetic compounds, and (ii) screening of this library on dermatological tests, in order to identify new biologically active compounds.

GREENPHARMA, located in the centre of FRANCE, is a technical platform specialised in natural products. The technical platform consists of three different services: one is specialised in plant extraction, the second in microplate development and the third in chemo-informatics. The plant extract service converts the plants supplied by our providers' network into extracts. The microplate service realises the development of our extract libraries and pure natural compound libraries in 96-well microplates. The chemo-informatics service develops databases allowing the management of the technical platform. Two products are produced: a pure and natural chemical library and an extract library made in a format compatible with high throughput screening. ADVANCELL, located in SPAIN, is a company specialised in the development of biological tests in order to identify new compounds in cosmetic and dermatological fields. These two companies are complementary in their activities. A collaboration of these two partners will allow common developments. The goal of this collaboration is twofold: the development of each partner, and acceleration of the identification of new active compounds such as cosmetics and therapeutics (i.e. products with high financial potentials). GREENPHARMA proposes, for this project, to develop a fourth service, which is compatible with the three existing services. This fourth service consists of the installation of a parallel chemistry system which will increase the molecular diversity of our chemical libraries. Indeed, we select the natural compounds according to their chemical diversity and their drug-likeness. This approach increases the probability of obtaining hits during a biological screening, but limits the quantity of selected compounds from the commercially available natural compounds. Moreover, the access to new original natural chemicals is limited by extraction and purification procedures which are quite difficult and expensive. For this reason, the combination of natural molecular diversity with the actual techniques of automated chemistry can easily increase the size of our libraries, in terms of molecular diversity. Some recent scientific publications confirm the viability of such a project. This will allow the rapid production of some original chemicals with high diversity and drug-like profile. After synthesis, the contribution of the other services, microplate and chemo-informatics, will allow the development of the hemi synthetic libraries and the corresponding databases. A complementary library will be developed. A specialist in parallel chemistry will be employed to undertake this activity. A part of the production will contribute to the development of GREENPHARMA whereas the other part will be transferred to our Spanish partner in order to screen all our hemi synthetic libraries on their biological tests. Biological results for each compound will be integrated in a database and analysed. During this project, we wish to focus on dermatological problems, especially skin invasive processes, such as viruses, bacteria and cancers. The selected hits can be optimised (ADMET) to ameliorate the putative candidate. All chemical derivatives of the candidate will be tested according to their activity, selectivity and toxicity. The best candidate, able to pass all these steps, will be patented. The pharmaco-chemistry design will be realised by the GREENPHARMA team whereas the biological part, selectivity, toxicity, etc. will be realised by the ADVANCELL team. Keywords: natural chemicals, dermatology, biological screening.
Acronym: 
NATCHEM
Project ID: 
2 885
Start date: 
15-05-2002
Project Duration: 
58months
Project costs: 
2 300 000.00€
Technological Area: 
Computational Chemistry and Modelling
Market Area: 
Pharmaceuticals/fine chemicals

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