Novel derivatives of deoxycholic acid bearing aliphatic or cyclic diamine moieties at the C-3 position: Synthesis and evaluation of anti-proliferative activity

Irina I. Popadyuk, Andrey V. Markov, Valeriya O. Babich, Oksana V. Salomatina, Evgeniya B. Logashenko, Marina A. Zenkova, Nariman F. Salakhutdinov

Результат исследования: Научные публикации в периодических изданияхстатья

4 Цитирования (Scopus)

Аннотация

A new library of deoxycholic acid derivatives bearing nitrogen-containing moieties at the C-3 position was synthesised from epoxy derivative 1 via an epoxide ring-opening reaction promoted by aliphatic or cyclic diamines and fully characterised by NMR and mass-spectroscopy. The synthesised compounds were screened for cytotoxicity against four human tumour cell lines. The results showed that some of the novel diamine-bearing derivatives displayed improved anti-proliferative activities over the parent compound DCA. Among them, a 1-methylpiperazine containing compound (6) showed promising activity and the highest selectivity against tumour cells of enterohepatic origin (HepG2: IC50 = 3.6 µM, SI = 9.0; HuTu-80: IC50 = 4.6 µM, SI = 6.9) and was identified as a lead molecule.

Язык оригиналаанглийский
Страницы (с-по)3755-3759
Число страниц5
ЖурналBioorganic and Medicinal Chemistry Letters
Том27
Номер выпуска16
DOI
СостояниеОпубликовано - 15 авг 2017

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