Comprehensive Survey of Chemical Libraries for Drug Discovery and Chemical Biology: 2008

摘要

This is the twelfth installment of the comprehensive survey series in combinatorial chemistry. Biologically active libraries reported in 2008 are captured in Tables 1 —5 under the headings of proteases, nonproteolytic enzymes, GPCRs, nonGPCRs, and oncolytics/antiinfectives. Table 6 lists molecular probes. Compound collections without disclosed biological activity are delineated in Tables 7—10 under the headings of scaffold derivatization/acyclic synthesis, monocyclic-, bicyclic/spirocyclic-, and polycyclic/macrocyclic synthesis. Polymer-supported reagents/scavengersflinkers are presented in Tables 11 (nonfluorous) and Table 12 (fluorous). There are 505 libraries and 30 molecular probes extracted from 490 literature citations. Approximately 90% of the citations originated from academic laboratories and ~80% of the chemical libraries relied on solution-phase synthesis for their preparation.