Synthesis and antitumor evaluation of (aryl)methyl-amine derivatives of dehydroabietic acid-based B ring-fused-thiazole as potential PI3K/AKT/mTOR signaling pathway inhibitors

In an attempt to search for new natural product-based antitumor agents, a series of novel (aryl)methyl-amine derivatives of dehydroabietic acid-based B ring-fused-thiazole were designed and synthesized. The primary bioassay showed that compounds 5r and 5s presented certain inhibitory activity agains...

Full description

Saved in:
Bibliographic Details
Published inMolecular diversity Vol. 25; no. 2; pp. 967 - 979
Main Authors Chen, Nai-Yuan, Xie, Yu-Lan, Lu, Guo-Dong, Ye, Fang, Li, Xin-Yu, Huang, Yu-Wen, Huang, Ming-Li, Chen, Tie-Yu, Li, Cui-Ping
Format Journal Article
LanguageEnglish
Published Cham Springer International Publishing 01.05.2021
Springer Nature B.V
Subjects
Antifungal agents
Binding sites
Biochemistry
Biomedical and Life Sciences
Life Sciences
Organic Chemistry
Original Article
Pharmacy
Polymer Sciences
Activity
Synthesis
Dehydroabietic acid
Thiazole
Antitumor
Online AccessGet full text

Cover

More Information
Summary:In an attempt to search for new natural product-based antitumor agents, a series of novel (aryl)methyl-amine derivatives of dehydroabietic acid-based B ring-fused-thiazole were designed and synthesized. The primary bioassay showed that compounds 5r and 5s presented certain inhibitory activity against cancer cells, weak cytotoxic activity against normal cells, and inhibitory activity against PI3K/AKT/mTOR signaling pathway. The binding modes and the binding site interactions between the active compounds and the target proteins were predicted preliminarily by the molecular docking method. Graphic abstract
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 14
content type line 23
ISSN:1381-1991
1573-501X
1573-501X
DOI:10.1007/s11030-020-10081-7