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Laboratory of Medicinal Chemistry

The laboratory has long-term experience in the field of anticancer agents. The research interest is focused in the design, synthesis and biological evaluation of new bioactive compounds with potential antitumor activity. Especially, modified steroidal derivatives, small heterocyclic compounds and natural products analogs (e.g. ecteinascidin/saframycin) are among the candidate synthetic targets. Members of the laboratory are in constant collaboration with Greek laboratories or teams in the University of Patras, in the Aristotle University of Thessaloniki and University of Athens as well as with members or teams of the National Hellenic Research Foundation in Athens. Also, members of the laboratory maintain research collaboration with partners in the EU. Our Laboratory has extensive experience in various chromatographic and spectrophotometric techniques for the purification and identification of all these compounds. Experience in drug design so that all these compounds turn out to be as active as possible (testing in collaboration with (Molecular) Biologists or Biochemists) toward the target (usually Receptor or Enzyme) and performing various reactions under inert conditions as needed, can also be considered as assets that our Laboratory can offer.

Research Team
Faculty members
Sotirios Nikolaropoulos, Professor , e-mail: This email address is being protected from spambots. You need JavaScript enabled to view it.
George Pairas, Associate Professor, e-mail: This email address is being protected from spambots. You need JavaScript enabled to view it.
Manolis Fousteris, Associate Professor, e-mail: This email address is being protected from spambots. You need JavaScript enabled to view it. [Lab. Director]

See our Lab Site here Research Activities/Expertise

  • Synthesis of heterocyclic steroids, synthesis of heterocyclic aromatic compounds (C. Camoutsis)
  • Synthesis of Homo-steroidal-esters of carboxylic derivatives of N,N-bis(2-chloroethyl)aniline and their Antitumor Activity (C. Camoutsis).
  • Synthesis of biologically and pharmacologically relevant molecules such as a- and b-amino acids, b-lactams, piperidines, and piperazines (P. Magriotis).
  • Total Synthesis of antitumor, antibiotic Natural Products (Cyclostreptin-(-)-FR182877, Ecteinascidin 743, Saframycin A, and Abyssomicin C) (P. Magriotis).
  • New Synthetic Methodology including novel routes to b-lactams and tetrasubstituted olefins (Tamoxifen analogs) (P. Magriotis).
  • Catalytic Enantioselective Synthesis of Substituted Piperazines as a general approach for the Construction of the Tetrahydroisoquinoline Antitumor Antibiotics (P. Magriotis).
  • Synthesis of ester and amide derivatives of anticancer agents with modified steroids (G. Pairas).
  • Computer aided design, synthesis and SAR studies of new compounds with biological activity (G. Pairas).
  • Design, synthesis and study of biological activity of antineoplasmatic drugs (S. Nikolaropoulos)
  • Design and synthesis of heterocyclic steroids (S. Nikolaropoulos)
  • Design and synthesis of small heterocyclic molecules as potential inhibitors of protein kinases (M. Fousteris).
  • Design, synthesis and evaluation of the biological activity of new steroidal alkylating agents (M. Fousteris).


Funded Research Projects

  • PENED 2003-Greek Secretariat of Research and Technology, 03ED756, “Synthesis, biological evaluation and structure-activity relationship study of new tetrahydroindole derivatives in the cardiovascular system”, Vice Coordinator Associate Professor Papapetropoulos Andreas, Co-coordinator Assistant Professor Nikolaropoulos Sotiris.


Recent Publications

  • I.R. Ezabadi, C. Camoutsis, P. Zoumpoulakis, A. Geronikaki, M. Sokovic, J. Glamocilija and A. Ciric, Sulfonamide-1,2,4-triazole derivatives as antifungal and antibacterial agents: Synthesis, biological evaluation, lipophilicity, and conformational studies, Bioorg. Med. Chem., 16, 1150 (2008).
  • A. Hussein, E. Mioglou- Kalouptsi, A. Papageorgiou, I. Karapidaki, Z. Iakovidou-Kritsi, Th. Lialiaris, E. Xrysogelou, C.H. Camoutsis and D. Mourelatos, Comparison of new nitrosoureas esters with modified steroidal nucleus for cytogenetic and antineoplastic activity, In Vivo, 21, 389 (2007).
  • A. Yiotakis, P.A. Magriotis, S. Vassiliou, A simple synthesis of the metabotropic receptor ligand (2S)-a-(Hydroxyymethyl)- glutamic acid and its Fmoc protected derivatives, Tetrahedron: Asymmetr., 18, 873 (2007).
  • S. Vassiliou, A. Yiotakis and P.A. Magriotis, efficient enantioselective synthesis of orthogonally protected (R)-a-alkylserines compatible with the solid phase peptide synthesis”, Tetrahedron Lett., 47, 7339 (2006).
  • S. Vassiliou and P.A. Magriotis, improved schöllkopf construction of quaternary a-amino acids: efficient enantioselective synthesis of integrin LFA-1 antagonist BIRT-377, Tetrahedron: Asymmetr., 17, 1754 (2006).
  • A.I. Koutsourea, M.A. Fousteris, E.S. Arsenou, A. Papageorgiou, G.N. Pairas and S.S. Nikolaropoulos, Rational design, synthesis, and in vivo evaluation of the antileukemic activity of six new alkylating steroidal esters, Bioorg. Med. Chem., 16, 5207 (2008).
  • G. Paloumbis, C.C. Petrou, B. Nock, T. Maina, G. Pairas, P.G. Tsoungas and P. Cordopatis, Synthesis of a protected δ-glyco-amino acid building block for incorporation into peptide chains, Synthesis, 6, 845 (2007).
  • S.-S. M. Vamvakas, L. Leondiadis, G. Pairas, E. Manessi-Zoupa, G.A. Spyroulias and P. Cordopatis, Expression, purification, and physicochemical characterization of the N-terminal active site of human angiotensin-I converting enzyme, J. Pept Sci., 13, 31 (2007).
  • M.A. Fousteris, A. Papakyriakou, A. Koutsourea, M. Manioudaki, E. Lampropoulou, E. Papadimitriou, G.A. Spyroulias and S.S. Nikolaropoulos, Pyrrolo[2,3-a]carbazoles as potential cyclin dependent kinase 1 (CDK1) inhibitors. Synthesis, biological evaluation, and binding mode through docking simulations, J. Med. Chem., 51, 1048 (2008).
  • M.A. Fousteris, A.I. Koutsourea, E.S. Arsenou, A. Papageorgiou, D. Mourelatos and S.S. Nikolaropoulos, Structure-antileukemic activity relationship study of B- and D-ring modified and nonmodified steroidal esters of 4-methyl-3-N,N-bis(2-chloroethyl)amino benzoic acid: a comparative study, Anti-Cancer Drugs, 18, 997 (2007).