Strategy, lead generation

Fejzo J, Lepre CA, Peng JW et al (1999) The SHAPES strategy an NMR-based approach for lead generation in drag discovery. Chem Biol 6(10) 755-769... 

An integrated approach to fragment-based lead generation philosophy, strategy and case studies from AstraZeneca s drug discovery programmes. Curr Top Med Chem 7, 1600-1629. 

To summarize this section, several research groups have effectively exploited parallels between SwAr strategies leading to [6,7]- and [6,6]-ben-zofused heterocycles and have described complementary reaction protocols suitable for generating diverse combinatorial libraries of benzothiazin-3-ones and quinoxalin-2-ones. 

Lead generation is the term applied to strategies developed to identify compounds which possess a desired but non-optimized biological (IUPAC). 

Gill, A. (2004). New lead generation strategies for protein-kinase inhibitors - fragment based screening approaches. Mini-Reviews in Medicinal Chemistry 4, 301-11. 

The second MCR development strategy leading to scaffold diversity involves MRS (Fig. 7), which is closely related to SRR but involves a versatile reactive intermediate that is generated from substrates A, B, and C by an initial MCR. This intermediate is then reacted in situ with a range of final differentiating components (D, E and F) to yield a diverse set of scaffolds. 

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