Synthesis of Physiological Active Compounds Laboratory

Alexander J. Misharin D.Sc., professor

CONTACTS

+7-(499)-246-58-20

Gelij V. Ponomarev D.Sc., professor

Mikhail S.Polyakov

Andrey M. Korolchuk

RESEARCH

Synthesis of physiologically active compounds laboratory is the oldest lab of IBMC, founded by famous soviet chemist academician M.M. Shemyakin in the 1945 year. A number of distinguished scientists such as M.N. Kolosov, V.K. Antonov, E.S. Chaman, V.F. Pozdnev, et al., worked in Laboratory over the years. All the time the area of the Laboratory research was design, synthesis, structural and biochemical investigation of novel physiological active compounds.

ACHIEVEMENTS

At present studies of Laboratory are focused on design, chemical synthesis, structural and biochemical investigation of novel derivatives of steroids and tetrapyrrolic macrocycles, as well as on their evaluation as potential anti-cancer agents.

  • Priority research in fields of antibiotics and amino acids (1945 – 1961)
  • Discovery of vitamin B6 and development of pyridoxal catalysis cornerstones (1951 – 1961)
  • Creation of original (the second in the world) peptide synthesizer and solid-phase synthesis of bradykinin (1966 – 1970)
  • Priority research in the fields of pyrocarbonates chemistry, synthesis of peptides and peptidomimetics (1969 – 2019), tetrapyrrolic macrocycles and related metallocomplexes (1990 – 2010), oxysterols and their analogs (2006 – 2010) 

PROJECTS

  • RSF grant 18-75-10008 (in collaboration with Blokhin Cancer Research Center)
  • RFBR grant 20-515-00021 Bel_а “ Design, synthesis and biological investigation of 21-norsteroid 20-аzoles as new antagonists of androgen and estrogen receptors in MCF-7 and LNCaP cells.

COMPLETED PROJECTS

  • RFBR grant 15-04-03970 “The role of membrane lipids in the aggregation of beta-amyloid (in collaboration with IMB RAN)
  • RFBR grant РФФИ 15-04-02939 “Novel nitrogen-containing derivatives of 17(20)E-pregnene as androgens metabolism regulators in prostate carcinoma cells”
  • RFBR grant 15-04-02426 “ Design and synthesis of bifunctional conjugates of pyropheophorbide a and their application for PDT of pathogens and tumors”
  • State contract № 14.N08.11.0107 «Preclinical investigation of pharmaceutical substance based on oxazolinyl derivative for prostate cancer therapy» 

Laboratory actively and fruitfully cooperates with Russian and foreign scientific institutions. Among the scientific collaborators of Laboratory are top researchers from:

  • Engelgardt Institute of Molecular Biology RAN
  • Zelinsky Institute of Organic Chemistry RAN
  • Pirogov Medical University
  • Blokhin Cancer Research Center
  • Research Institute of Macroheterocycles (Ivanovo State University of Chemistry and Technology)
  • Institute of Bioorganic chemistry NANB (Minsk, Belarus)
  • Palacky University and Institute of Experimental Botany AS CR (Olomouc, Chech Republic)

The laboratory is a platform for student’s scientific works and performing of baccalaureate, magisterial and diploma projects of graduates from Mendeleev University of Chemical Technology, Moscow Technological University, Pirogov Medical University 

List of Student’s Projects Performed in Laboratory (2016–2020)

  • Zazulina О.V. «Synthesis of main steroid blocks for the preparation of antiandrogens» (baccalaureate work, Mendeleev University of Chemical Technology, 2016.)
  • Yanova Т.I. “Biological activity of biosynthetic precursors of brassinosteroids and related derivatives as potential anti-tumor agents (diploma work, Pirogov Medical University, 2017.)
  • Zazulina О.V. «Synthesis of nitrogen containing derivatives of 17β-hydroxypregnanic and 17α-hydroxypregnanic acids – novel potential antiandrogens» (magisterial dissertation, Mendeleev University of Chemical Technology 2018)
  • Taratynova М. О. «Novel polyfunctional conjugates of testosterone with pyropheophorbide a – synthesis and biological activity» (baccalaureate work, Moscow Technological University, 2018)
  • Latysheva А.S. «Inhibition of 17α-hydroxylase/17,20-lyase by nitrogen containing derivatives of [17(20)E]-pregnene» (diploma work, Pirogov Medical University, 2018)
  • Scherbakov S.А. «Synthesis of nitryl and oxazolinyl derivatives of Δ16-pregnene – new potential antiandrogens» (baccalaureate work, Mendeleev University of Chemical Technology, 2018)
  • Меstahudinova J.А. «Synthesis of steroid blocks for preparation of new inhibitors of Hh- signaling» (baccalaureate work, Mendeleev University of Chemical Technology, 2020)
  • Маtiusova Е.V. «Synthesis of seco-D-androstane and seco-D-21-norpregane derivatives – precursors for the preparation of new antiandrogens» (baccalaureate work, Mendeleev University of Chemical Technology, 2020)

Ph.D. Theses Prepared in the Laboratory

  • Zolottsev V. A. ” Synthesis of nitrogen-containing derivatives of the pregnane series - potential antitumor agents ” (02.00.03 –Organic chemistry, 2019 г.)
  • Pregn-17(20)-еne derivatives exhibited anti-tumor activity. Patent RU2015111223A.
  • Pharmaceutical composition for luminescent diagnostics of pathologic alterations of skin and mucosa. Patent RU2016107576A
  • Method of obtaining diethrye salt 2,4-di(1-metoxyethyl)deuteroporphyrin-IX (Dimegin). Patent RU2647588 C1.
  • Photosensitizer for therapy of oncologic diseases and the method of its preparation. Patent RU2646477C1.
  • Method of preparation of dikalium salt ytterbium complex of 2,4-di(1-metoxyethyl)deuteroporphyrin-IX acetyl acetonate Patent RU2697418 С1.