Concise and diversity-oriented synthesis of novel scaffolds embedded with privileged benzopyran motif.
A branching DOS strategy for an unbiased natural product-like library with embedded privileged benzopyran motif was established to provide complexity and diversity of resulting heterocycles with desired drug-likeness. The importance of skeletal diversity conducted on a privileged substructure was demonstrated through the biological evaluation of a small molecule library representing 22 unique core skeletons via in vitro cytotoxicity assay.
Ko
Sung Kon
SK
School of Chemistry, Seoul National University, Seoul, 151-747, Korea.
Jang
Hwan Jong
HJ
Kim
Eunha
E
Park
Seung Bum
SB
D001578:Benzopyrans / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D049109:Cell Proliferation / Q000187:drug effects; D002626:Chemistry, Pharmaceutical / Q000379:methods* / Q000639:trends; D020650:Combinatorial Chemistry Techniques; D020128:Inhibitory Concentration 50; D008175:Lung Neoplasms / Q000188:drug therapy; D008956:Models, Chemical; D008968:Molecular Conformation; D015394:Molecular Structure; D004364:Pharmaceutical Preparations; D014407:Tumor Cells, Cultured / Q000187:drug effects
D001578:Benzopyrans; D004364:Pharmaceutical Preparations