Ontology highlight
ABSTRACT:
SUBMITTER: Bachovchin KA
PROVIDER: S-EPMC6556231 | biostudies-literature | 2019 Jan
REPOSITORIES: biostudies-literature
Bachovchin Kelly A KA Sharma Amrita A Bag Seema S Klug Dana M DM Schneider Katherine M KM Singh Baljinder B Jalani Hitesh B HB Buskes Melissa J MJ Mehta Naimee N Tanghe Scott S Momper Jeremiah D JD Sciotti Richard J RJ Rodriguez Ana A Mensa-Wilmot Kojo K Pollastri Michael P MP Ferrins Lori L
Journal of medicinal chemistry 20190110 2
Lapatinib, an approved epidermal growth factor receptor inhibitor, was explored as a starting point for the synthesis of new hits against Trypanosoma brucei, the causative agent of human African trypanosomiasis (HAT). Previous work culminated in 1 (NEU-1953), which was part of a series typically associated with poor aqueous solubility. In this report, we present various medicinal chemistry strategies that were used to increase the aqueous solubility and improve the physicochemical profile withou ...[more]