Total synthesis of natural products:

• (+)-Biotin, one of the water-soluble B-vitamins. (+)-Biotin plays an essential role as coenzyme in carboxylation reactions related to biochemical processes such as fatty acid biosynthesis and gluconeogenesis. It is used as feed additive to correct deficiencies in poultry and swine caused by a lack of (+)-Biotin.

• Himbacine and its analogues. Himbacine, isolated from Galbulimina Baccata can serve as a potential agent against Alzheimer's disease. In order to establish structure-activity relationships, it is necessary to synthesize analogues of this molecule.

• 11-oxygenated steroids.

• (-)-Periplanone-B, is the major sex pheromone component of the American cockroach (Periplaneta americana). The potent attractant activity of this compound can make it a efficient and selctive 'pheromone insecticide'.

The search for analogues of natural products:

• 1,25-dihydroxyvitamin D3; different projects concerning the synthesis of new analogues of 1,25-dihroxyvitamin D3 are currently undertaken. The use of these derivatives lies in the field of cancer healing.

• Himbacine; please see the part about the total synthesis of natural products.

• Based on a combination of the steroidal skeleton of estradiol and a enediyne moiety, novel cycloaromatisation precursors as potential selective antitumor agents are developed.

Research concerning biochemical processes:

• The synthesis of serine-protease mimics by 'classic' (solution phase) and by combinatorial chemistry. In order to have a better understanding of the principles of catalysis in serine-proteases, research is done to mimic the active site of the enzyme.

• Efforts are also done to synthesize epoxysqualene-like polyenes. The cyclization of these polyenes should help to elucidate the mechanism(s) of the enzymes that accomplish these transformations in Nature.

• Further development of the syntheses of 1,25-dihydroxyvitamin D3 analogues with the aim of establishing structure-activity relationships.

• The search for himbacine analogues.

• The total syntheses of (+)-Biotin, 11-oxygenated steroids and (-)-Periplanone-B.

• Studies in the field of biochemical processes: mimics of the active site of serine-proteases by 'classic' and by combinatorial chemistry. Ongoing research in the epoxysqualene-like polyenes synthesis and their cyclization behaviour.

• Development of novel strategies for the construction of chemical libraries via combinatorial chemistry.

• "Application of combinatorial procedures in the search for serine-protease-like activity with focus on the acyl transfer step."
  H. De Muynck, A. Madder, N. Farcy, P. J. De Clercq, M. N. Pérez-Payan, L. M. Öhberg, A. P. Davis
  Angew. Chem. Int. Ed. 2000 , 39 , 145-148.

• "A novel sensitive colorimetric assay for visual detection of solid phase bound amines."
  A. Madder, N. Farcy, N. G. C. Hosten, H. De Muynck, P. J. De Clercq, J. Barry, A. P. Davis
  Eur. J. Org. Chem. 1999 , 2787-2791.

• "Synthesis, biological activity and conformational analysis of four seco-D-15,19-bisnor-1a,25-dihydroxyvitamin D analogs, diastereomeric at C17 and C20."
  X. Zhou, G.-D. Zhou, D. Van Haver, M. Vandewalle, P. J. De Clercq, A. Verstuyf, R. Bouillon J. Med. Chem. 1999 , 42 , 3539-3556.

• "On the use of volume maps in the conformational analysis of vitamin D analogs."
  D. Van Haver, P. J. De Clercq
  Bioorg. & Med. Chem. Lett. 1998 , 8 , 1029-1034.

• "Stepwise approach toward first genaration nonenzymatic hydrolases."
  A. Madder, P. J. De Clercq, J.-P. Declercq
  J. Org. Chem. 1998 , 63 , 2548-2559.

• "Studies Directed Towards the Total Synthesis of (+)-Himbacine."
  S. Hofman, G. De Baecke, B. Kenda, P. De Clercq
  Synthesis 1998 , 479-489.

• "Biotin: A Timeless Challenge for Total Synthesis." Pierre J. De Clercq
  Chem. Rev. 1997 , 97 , 1755-1792.

• "Estramycins: a new diyl precursor family derived from estradiol."
  Jing Wang, P. J. De Clercq
  Angew. Chem. Int. Ed. 1995 , 34 , 1749-1752.

• "Polyene cyclizations related to oxidosqualene cyclization. A model for the anti- Markovnikov closure of ring C."
  K. Berckmoes, P. J. De Clercq, D. Viterbo
  J. Am. Chem. Soc. 1995 , 117 , 5857-5858.

• "Novel enantioselective syntheses of (+)-biotin."
  F. D. Deroose, P. J. De Clercq
  J. Org. Chem. 1995 , 60 , 321-330.

• "Intramolecular Diels-Alder reaction with furan-diene: syntheses of gibberellins (+)-GA1 and (+)-GA3."
  F. Nuyttens, J. Hoflack, G. Appendino, P. J. De Clercq. Synlett 1995 , 105-107.

• "The influence of anchoring substitution in 1,3-amino alcohols on the rate and mechanism of esterification by acetylimidazole and by p-nitrophenyl acetate."
  I. Steels, P. J. De Clercq, H. Maskill
  J. Chem. Soc. Chem. Commun. 1993 , 294-295.
  

• Hilde De Muynck (2000): "De ontwikkeling van modelverbindingen voor serineproteasen via combinatorische technieken".

• Christel Meert (2000): "De ontwikkeling van nieuwe cycloaromatisatieprecursoren op basis van oestradiol".

• Sven Hofman (2000): "Synthese van H-himbacine, een muscarinereceptor antagonist".

• S. Gabriëls (2000): "Ontwikkeling van analogen van vitamine D3 met opgelegde zijketenoriëntatie".

• M. Sey (2000): "Studie van cyclisatie van conformationeel verankerde analogen van squaleen".

• A. Madder (1997): "Stapsgewijze ontwikkeling van niet-enzymatische hydrolasen".

• X. Zhou (1997): "A symmetric synthesis of 1a,25-dihydroxyvitamin D analogs modified in the C-ring".

• K. Berckmoes (1997): "Synthese van cyclisatie van modelverbindingen van 2,3-epoxysqualeen".

• G. De Baecke (1995): "Bijdrage tot de totaalsynthese van himbacine".

• J. De Schrijver (1994): "Studie voor de totaalsynthese van 1(S),25-dihydroxyvitamine D3 derivaten met opbouw van de A-ring via Diels-Alderreactie van een furan-dieen en een alleen-diënofiel".

• F. Deroose (1994): "Studie voor de totaalsynthese van (+)-biotin".

• J. Wang (1994): "The synthesis of novel cycloaromatization precursors incorporating estradiol".

• T. De Geyter (1994): "Studie van de totaalsynthese van (-)-periplanon-B".

• I. Steels (1993): "Studie van het gebruik van verankerde groepen bij het ontwerpen van modelverbindingen van serineproteasen en chirale inductoren voor de stereoselectieve reductie van prochirale ketonen".

• Z.-G. Dong (1993): "Synthesis of fluorine substituted and of D-ring modified analogues of vitamin D for modulation of the biological activity".

• F. De Corte (1992): "Studie van het gebruik van verankerde groepen bij het ontwerp van chirale inductoren en bij de beïnvloeding van de intramoleculaire Diels-Alderreactiviteit".

• J. Hoflack (1991): "Deel I. Computermethode voor het conformationeel onderzoek van polycyclische verbindingen uitgaande van hun tweedimensionaal structuur-diagram. Deel II. Inleidende studie voor een biomimetische totaalsynthese van gibberelline-plantgroeihormonen via intramoleculaire Diels-Alderreactie met furan-diënen".