Ontology highlight
ABSTRACT:
SUBMITTER: Lukesh JC
PROVIDER: S-EPMC5599373 | biostudies-literature | 2017 Sep
REPOSITORIES: biostudies-literature
Lukesh John C JC Carney Daniel W DW Dong Huijun H Cross R Matthew RM Shukla Vyom V Duncan Katharine K KK Yang Shouliang S Brody Daniel M DM Brütsch Manuela M MM Radakovic Aleksandar A Boger Dale L DL
Journal of medicinal chemistry 20170831 17
A series of 180 vinblastine 20' amides were prepared in three steps from commercially available starting materials, systematically exploring a typically inaccessible site in the molecule enlisting a powerful functionalization strategy. Clear structure-activity relationships and a structural model were developed in the studies which provided many such 20' amides that exhibit substantial and some even remarkable enhancements in potency, many that exhibit further improvements in activity against a ...[more]