Synthesis and biological evaluation of novel farnesylthiosalicylic acid derivatives for cancer treatment

Autor:	Yong, Ling, Xuemin, Wang, Hongyan, Zhu, Zhiqiang, Wang, Chenjun, Xu, Xinyang, Wang, Li, Chen, Wei, Zhang
Rok vydání:	2013
Předmět:	Dose-Response Relationship Drug Molecular Structure MAP Kinase Signaling System Blotting Western Antineoplastic Agents Apoptosis Flow Cytometry Farnesol Salicylates Inhibitory Concentration 50 Structure-Activity Relationship Cell Line Tumor Drug Design ras Proteins Humans
Zdroj:	Archiv der Pharmazie. 347(5)
ISSN:	1521-4184
Popis:	Novel farnesylthiosalicylic acid (FTS) derivatives were synthesized by coupling with different substituted diamines. Their in vitro growth inhibitory activities against seven human cancer cell lines were evaluated. The results revealed that the synthetic farnesylthiosalicylamides displayed significant antitumor activities compared to the positive control FTS. Especially, compound 8f exhibited the strongest antitumor activities with IC50 values of 6.20-7.83 µM, which were one- to threefold less than those of sorafenib and six- to tenfold less than that of FTS against each cell line in vitro. Furthermore, 8f could inhibit the Ras-related signaling pathway and induce SMMC-7721 cell apoptosis superior to FTS in a dose-dependent manner. These data indicate that 8f may hold greater promise as therapeutic agent for the intervention of human cancers.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=pmid________::99376054ef49c5e7688afcc893f63896 https://pubmed.ncbi.nlm.nih.gov/24435839 Zobrazit plný text záznamu Plný text