scholarly journals Tryptophanol-Derived Oxazolopyrrolidone Lactams as Potential Anticancer Agents against Gastric Adenocarcinoma

2021 ◽  
Vol 14 (3) ◽  
pp. 208
Author(s):  
Margarida Espadinha ◽  
Valentina Barcherini ◽  
Lídia M. Gonçalves ◽  
Elies Molins ◽  
Alexandra M. M. Antunes ◽  
...  

Gastric cancer is one of the deadliest cancers in modern societies, so there is a high level of interest in discovering new drugs for this malignancy. Previously, we demonstrated the ability of tryptophanol-derived polycyclic compounds to activate the tumor suppressor protein p53, a relevant therapeutic target in cancer. In this work, we developed a novel series of enantiomerically pure tryptophanol-derived small molecules to target human gastric adenocarcinoma (AGS) cells. From an initial screening of fourteen compounds in AGS cell line, a hit compound was selected for optimization, leading to two derivatives selective for AGS gastric cells over other types of cancer cells (MDA-MB-231, A-549, DU-145, and MG-63). More importantly, the compounds were non-toxic in normal cells (HEK 293T). Additionally, we show that the growth inhibition of AGS cells induced by these compounds is mediated by apoptosis. Stability studies in human plasma and human liver microsomes indicate that the compounds are stable, and that the major metabolic transformations of these molecules are mono- and di-hydroxylation of the indole ring.

2007 ◽  
Vol 257 (1) ◽  
pp. 56-64 ◽  
Author(s):  
Cheng-Yun Jin ◽  
Cheol Park ◽  
JaeHun Cheong ◽  
Byung Tae Choi ◽  
Tae Ho Lee ◽  
...  

2014 ◽  
Vol 9 (9) ◽  
pp. 1934578X1400900
Author(s):  
Kentaro Tsukahara ◽  
Kazufumi Toume ◽  
Hanako Ito ◽  
Naoki Ishikawa ◽  
Masami Ishibashi

The antibiotic β-indomycinone was isolated from Streptomyces sp. IFM11607 by cytotoxicity-guided fractionation against human gastric adenocarcinoma AGS cells, and the geometry of its Δ17,18-double bond was revised from E to Z based on the coupling constant.


2008 ◽  
Vol 18 (1) ◽  
pp. 120-128 ◽  
Author(s):  
Jae-Jun Lee ◽  
Dong-Hyuk Shin ◽  
Sang-Eun Park ◽  
Won-Il Kim ◽  
Dong-Il Park ◽  
...  

2015 ◽  
Vol 06 (11) ◽  
pp. 496-501 ◽  
Author(s):  
Yanchao Liu ◽  
Qiliang Qin ◽  
Agula Bo ◽  
Hairong Zhang ◽  
Qing Zhang ◽  
...  

2011 ◽  
Vol 102 (3) ◽  
pp. 549-556 ◽  
Author(s):  
Young-Cheol Lim ◽  
Je-Ok Yoo ◽  
Seong-Sik Kang ◽  
Young-Myeong Kim ◽  
Kwon-Soo Ha

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