Design, synthesis, and biological activities of madindoline analogues.
A research program is under way to develop a series of madindoline-based inhibitors targeting interleukin 6. Such inhibitors will have potential use in fighting a variety of diseases for which no effective therapeutic drugs currently exist. Madindoline is no longer available from natural sources. Consequently, we have developed a purely synthetic route to ensure a supply of the compound. The synthesis of a range of analogues is described, all of which were evaluated for their inhibitory activity against the growth of IL-6-dependent 7TDI cells. From these assays, several synthetic madindoline analogues were identified as highly promising candidates for further development.
Yamamoto
Daisuke
D
The Kitasato Institute, and Kitasato Institute for Life Sciences and Graduate School of Infection Control Sciences, School of Pharmaceutical Sciences, Kitasato University, Japan.
Sunazuka
Toshiaki
T
Hirose
Tomoyasu
T
Kojima
Naoto
N
Kaji
Eisuke
E
Omura
Satoshi
S
D000818:Animals; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000138:chemical synthesis* / Q000494:pharmacology*; D002460:Cell Line; D015195:Drug Design; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D051379:Mice
D019086:Bridged Bicyclo Compounds, Heterocyclic; D007211:Indoles; C103158:madindoline A