Tubulin targeted antimitotic agents based on adamantane lead compound: synthesis, SAR and molecular modelingстатья
Информация о цитировании статьи получена из
Web of Science,
Scopus
Статья опубликована в журнале из списка Web of Science и/или Scopus
Дата последнего поиска статьи во внешних источниках: 2 сентября 2020 г.
Аннотация:5-Hydroxymethyl-2-methoxyphenyl adamantane-1-acetate inhibits cell proliferation and stimulates depolymerization of microtubules of cancer cells to free tubulin. A series of its analogs was synthesized via Steglich esterification or Mitsunobu reaction to determine the role of structural subunits of the molecule in tubulin binding. The structure – activity relationship (SAR) studies led to the discovery of 1-[2-(5-(hydroxymethyl)-2-methoxyphenyl)ethyl]adamantane, which exhibits a dual-target profile and retains in vitro activity observed for the lead-compound, but is more stable metabolically.
Мол. + РНФ.