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Laboratory for Biologically Active Compounds

#3582


The Creation of Laboratory for Biologically Active Compounds Synthesis and Investigation Oriented to the Development of Combinatorial Chemistry

Tech Area / Field

  • MED-DRG/Drug Discovery/Medicine
  • AGR-VTH/Vaccines and Theraupetics/Agriculture
  • CHE-IND/Industrial Chemistry and Chemical Process Engineering/Chemistry
  • CHE-SYN/Basic and Synthetic Chemistry/Chemistry

Status
3 Approved without Funding

Registration date
04.08.2006

Leading Institute
Russian Scientific Center of Applied Chemistry, Russia, St Petersburg

Collaborators

  • Max Plank Institute of Molecular Plant Physiology, Germany, Potsdam-Golm\nChemical Diversity Inc., USA, CA, San Diego

Project summary

Heterocyclic compounds remain the most prospective class of biologically active substances being used in chemical and pharmaceutical industry, veterinary. Wide-area combinatory synthesis of various derivatives of a row of heterocyclic compounds and testing their biological activity is scheduled to carry out in the project.

Purposes and tasks of the project are:

  1. The creation of the laboratory of synthesis of biologically active substances oriented to the development of combinatory chemistry to perform the orders of Russian and foreign chemical- pharmaceutical companies.
  2. To elaborate the methods of synthesis of basic compounds based on triazolopyrimidines, pyrazinopyrimidines, quinoxalines, oxadiazols etc. (Fig.1)
  3. To synthesize a series of representative compounds meeting the common formulas presented in Fig.1. (no less than 100 compounds of each type).
  4. To conduct biological tests of obtained compounds on the panel of actual, pharmaceutically significant biological targets belonging to families of kinase enzymes and/or receptors coupled with G-proteins.

Project participants

The project will be realized in FSUP “RSC “Applied chemistry” in which a scientific and technical, intellectual potential of chemists before being occupied with defense investigations remained intact (ISTC code - 1.1.). Since 1994 organic chemists of the centre a number of contracts on synthesis and development of production technologies for complex organic compounds including drugs and their semi-products has been accomplished. The implementation of the given project will provide the obtaining new scientific knowledge in combinatory chemistry and biotechnology and also will promote solution of scientific and organization problems and give a start for the creation of one of the first modern laboratories with a high part of participation of former defense scientists able to self-dependent operation in market economics conditions and oriented to the accomplishment of high-technology orders of Russian and foreign chemical, pharmaceutical and biotechnical companies in Saint-Petersburg.

Results of the project and their commercialization

As a result of project realization the effective methods of synthesis of the above compounds (structures I-IV) allowing to obtain both large series of compounds in a scale of 100-200 mg (no less than 100 structures in each) and preparative quantities of compounds in a scale of 1-10 kg will be developed. When using these methods the representative libraries of the specified compounds in quantity sufficient for realization of primary biological tests (50-100 mg) will be obtained. Besides, the synthesized compounds will be tested by a method of high-productive biological screening on the activity with respect to a row of pharmaceutical-significant bio-targets.

Field and forms of possible use of the results

The resulting compounds and information are intended for using by special state and commercial organizations working in the area of development and introduction of chemical- pharmaceutical substances to production. Active compounds discovered at the primary screening stage then can be examined by the specified organizations with the object to detection of the following properties:

  • activity with respect to different lines of tumour cells;
  • activity to animals (pre-clinical tests);
  • activity to human patients (clinical tests);
  • pharmacokinetic properties; pharmacodynamic properties; toxicity etc.

The substances produced by means the developed project can be prototypes of new drug-likeness acting on specific bio-targets; as such they are a prospective object of investigations and commercialization for companies and organizations being occupied in the area of development of new drugs-likeness and the study of mechanisms of their effect. Besides, using results of the investigations it is planned to publish to 3 scientific articles, 1-2 applications for a patent and 1-2 Ph.D. theses.

Fig. 1. Compounds being an object of the present project.


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