Structure–Activity Relationships of α-, β1-, γ-, and δ-Tomatine and Tomatidine against Human Breast (MDA-MB-231), Gastric (KATO-III), and Prostate (PC3) Cancer Cells

2012 ◽  
Vol 60 (15) ◽  
pp. 3891-3899 ◽  
Author(s):  
Suk Hyun Choi ◽  
Jun-Bae Ahn ◽  
Nobuyuki Kozukue ◽  
Hyun-Jeong Kim ◽  
Yosuke Nishitani ◽  
...  
2009 ◽  
Vol 53 (7) ◽  
pp. 845-858 ◽  
Author(s):  
Rosamaria Lappano ◽  
Camillo Rosano ◽  
Antonio Madeo ◽  
Lidia Albanito ◽  
Pierluigi Plastina ◽  
...  

2014 ◽  
Vol 82 ◽  
pp. 565-573 ◽  
Author(s):  
Safiye Emirdağ-Öztürk ◽  
Tamer Karayıldırım ◽  
Aysun Çapcı-Karagöz ◽  
Özgen Alankuş-Çalışkan ◽  
Ali Özmen ◽  
...  

2007 ◽  
Vol 17 (13) ◽  
pp. 3722-3728 ◽  
Author(s):  
Toshiaki Hasegawa ◽  
Jiao Bai ◽  
Jungui Dai ◽  
Liming Bai ◽  
Junichi Sakai ◽  
...  

Cancers ◽  
2020 ◽  
Vol 12 (4) ◽  
pp. 875 ◽  
Author(s):  
Korrakod Petsri ◽  
Masashi Yokoya ◽  
Sucharat Tungsukruthai ◽  
Thanyada Rungrotmongkol ◽  
Bodee Nutho ◽  
...  

Myeloid cell leukemia 1 (Mcl-1) and B-cell lymphoma 2 (Bcl-2) proteins are promising targets for cancer therapy. Here, we investigated the structure–activity relationships (SARs) and performed molecular docking analysis of renieramycin T (RT) and its analogues and identified the critical functional groups of Mcl-1 targeting. RT have a potent anti-cancer activity against several lung cancer cells and drug-resistant primary cancer cells. RT mediated apoptosis through Mcl-1 suppression and it also reduced the level of Bcl-2 in primary cells. For SAR study, five analogues of RT were synthesized and tested for their anti-cancer and Mcl-1- and Bcl-2-targeting effects. Only two of them (TM-(–)-18 and TM-(–)-4a) exerted anti-cancer activities with the loss of Mcl-1 and partly reduced Bcl-2, while the other analogues had no such effects. Specific cyanide and benzene ring parts of RT’s structure were identified to be critical for its Mcl-1-targeting activity. Computational molecular docking indicated that RT, TM-(–)-18, and TM-(–)-4a bound to Mcl-1 with high affinity, whereas TM-(–)-45, a compound with a benzene ring but no cyanide for comparison, showed the lowest binding affinity. As Mcl-1 helps cancer cells evading apoptosis, these data encourage further development of RT compounds as well as the design of novel drugs for treating Mcl-1-driven cancers.


2003 ◽  
Vol 46 (25) ◽  
pp. 5402-5415 ◽  
Author(s):  
Jan Šarek ◽  
Jiří Klinot ◽  
Petr Džubák ◽  
Eva Klinotová ◽  
Věra Nosková ◽  
...  

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