scholarly journals A Review of the Structure–Activity Relationship of Natural and Synthetic Antimetastatic Compounds

Biomolecules ◽  
2020 ◽  
Vol 10 (1) ◽  
pp. 138 ◽  
Author(s):  
Liew ◽  
Malagobadan ◽  
Arshad ◽  
Nagoor

There are innumerable anticancer compounds derived from either natural or synthetic origins. Many of these compounds have been further developed through structural modifications to not only inhibit cancer cell growth but also to exert an antimetastatic effect. This is achieved by attaching different substituents to generate different structure–activity relationships. This review highlights the effectiveness of different functional groups known to have antimigration and antiproliferation activities, such as fluoro, methoxy, methyl, amino, hydroxy, nitro, bromo, chloro, methylamino, ethoxy, carbonyl, iodo, and trifluoromethyl groups. Additionally, the positioning of these functional groups plays an important role in their anticancer activities, which was evident in one of our studies comparing analogues of a natural compound. Thus, this review suggests future recommendations for the design and development of improved anticancer drugs with higher efficacy.

2010 ◽  
Vol 16 (5) ◽  
pp. 242-248 ◽  
Author(s):  
Masakatsu Kamiya ◽  
Keisuke Oyauchi ◽  
Yoshinori Sato ◽  
Takuya Yokoyama ◽  
Mofei Wang ◽  
...  

2017 ◽  
Vol 26 (10) ◽  
pp. 2624-2638 ◽  
Author(s):  
Ahmed H. Halawa ◽  
Mahmoud M. Elaasser ◽  
Ahmed M. El Kerdawy ◽  
Ahmed M. A. I. Abd El-Hady ◽  
Hassein A. Emam ◽  
...  

RSC Advances ◽  
2015 ◽  
Vol 5 (89) ◽  
pp. 73290-73300 ◽  
Author(s):  
Bao Tu ◽  
Zhi-Feng Chen ◽  
Zhi-Juan Liu ◽  
Rong-Rong Li ◽  
Yu Ouyang ◽  
...  

The influence of functional groups on the interaction has been studied detailed here; fluorescence quenching degrees and the conformation change are considered through multiple methods; molecular docking has been introduced to verify related results.


2020 ◽  
Vol 21 (7) ◽  
pp. 2467 ◽  
Author(s):  
Catarina Pimpão ◽  
Inês V. da Silva ◽  
Andreia F. Mósca ◽  
Jacinta O. Pinho ◽  
Maria Manuela Gaspar ◽  
...  

Polyoxometalates (POMs) are of increasing interest due to their proven anticancer activities. Aquaporins (AQPs) were found to be overexpressed in tumors bringing particular attention to their inhibitors as anticancer drugs. Herein, we report for the first time the ability of polyoxotungstates (POTs), such as of Wells–Dawson P2W18, P2W12, and P2W15, and Preyssler P5W30 structures, to affect aquaporin-3 (AQP3) activity and impair melanoma cell migration. The tested POTs were revealed to inhibit AQP3 function with different effects, with P2W18, P2W12, and P5W30 being the most potent (50% inhibitory concentration (IC50) = 0.8, 2.8, and 3.2 µM), and P2W15 being the weakest (IC50 > 100 µM). The selectivity of P2W18 toward AQP3 was confirmed in yeast cells transformed with human aquaglyceroporins. The effect of P2W12 and P2W18 on melanoma cells that highly express AQP3 revealed an impairment of cell migration between 55% and 65% after 24 h, indicating that the anticancer properties of these compounds may in part be due to the blockage of AQP3-mediated permeability. Altogether, our data revealed that P2W18 strongly affects AQP3 activity and cancer cell growth, unveiling its potential as an anticancer drug against tumors where AQP3 is highly expressed.


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