Design, synthesis and bioactivities evaluation of novel oleanolic acid derivatives as potent PI3K inhibitors

Autor:	Yan-Ling, Song, Ming-Xia, Zhu, Hai-Feng, Wang, Yan-Qiu, Meng
Rok vydání:	2022
Předmět:	Pharmacology Complementary and alternative medicine Organic Chemistry Drug Discovery Pharmaceutical Science Molecular Medicine General Medicine Analytical Chemistry
Zdroj:	Journal of Asian Natural Products Research. 25:264-276
ISSN:	1477-2213 1028-6020
DOI:	10.1080/10286020.2022.2066528
Popis:	Oleanolic acid has previously been shown to possess PI3K inhibitory activity, thus, the purpose of this work was to generate a series of derivatives that improve the potency. Twenty rationally designed oleanolic acid derivatives were synthesized and tested the cytotoxicity and PI3K inhibitory activity. The results suggested that attachment of additional structural elements such as association of thiazole group to A ring and insertion of phenylurea group was important for increasing activities. The most active derivative was compound
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::17050e21251206d7f2f0526e2a3940df https://doi.org/10.1080/10286020.2022.2066528 Zobrazit plný text záznamu