Heterocycles high-throughput screening

In recent years, developments in high-throughput screening inspired many pharmaceutical companies to focus and rely on combinatorial chemistry, especially massive parallel synthesis, to find new lead structures. The employed chemistry is often simple and the concept depends on sheer numbers for success. The main research areas were heterocyclic and peptide chemistry, and the resulting structures often lacked complexity and diversity, and most importantly the chance to utilize the evolutionary advantage of natural products with their privileged structures. 

Westman, J. and Orrling, K., Cascade synthesis with (triphenylphosphoranylidene)-ethenone as a versatile reagent for fast synthesis of heterocycles and unsaturated amides under microwave dielectric heating, Comb. Chem. High Throughput Screening, 2002, 5, 571-574. 

In conclusion, it is clear that the S, Ar approach to benzofused heterocycles can provide pharmaceutically attractive compounds for high-throughput screening. We anticipate that useful lead molecules will emerge from these studies and look forward to reporting new correlations between bioactivities and molecular structure. 

Chauhan, P.M. (2001) Recent development in the combinatorial synthesis of nitrogen heterocycles using solid phase technology. Combi. Chem. High Throughput Screening 4 35-51. 

Andres, C.J., Denhart, D.J., Deshpande, M.S. and Gillman, K.W. (1999) Recent advances in the solid phase synthesis of drug-like heterocyclic small molecules. Comb. Chem. High Throughput Screen 2 191-210. 

Knepper, K., GU, C., and Brase, S., Natural product-like and other biologically active heterocyclic libraries using solid-phase techniques in the post-genomic era, Comb. Chem. High Throughput Screen., 6, 673, 2003. 

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