Design and Synthesis of Amide Derivatives of Melampomagnolamine: Acted as Potent Anti-cancer Agents

Author(s):  
Venumadhav Janganati
2011 ◽  
Vol 46 (8) ◽  
pp. 3210-3217 ◽  
Author(s):  
Doma Mahendhar Reddy ◽  
Naveed A. Qazi ◽  
Sanghpal D. Sawant ◽  
Abid H. Bandey ◽  
Jada Srinivas ◽  
...  

2020 ◽  
Vol 5 (39) ◽  
pp. 12317-12319
Author(s):  
Narasimha Swamy Thirukovela ◽  
Satheesh Kumar Nukala ◽  
Narsimha Sirassu ◽  
Ravinder Manchal ◽  
Prasad Gundepaka ◽  
...  

Author(s):  
Liwaliding Maihesuti ◽  
Hongwei Gao ◽  
Qi Wang ◽  
Jianguo Cao ◽  
Haji Akber Aisa ◽  
...  

Background: Flavonolignans like silybin, hydnocarpin, and siliandrin are a group of natural compounds combining the structural moieties of flavonoid and phenylpropanoid (lignan). Hydnocarpin and silandrin were less explored because of trace occurrence in nature. Objective: The present study aimed to develop a chemical conversion of silybin to hydnocarpin, and siliandrin. Also, a series of amide derivatives would be synthesized and biologically evaluated with regard to their anti-cancer effects. Methods: In order to selectively convert silybin to 23-iodo silybin, 23-iodo hydnocarpin D and 23-iodo isosilandrin, the ratio of Ph3P, imidazole and molecular iodine was meticulously adjusted. These three iodide compounds were converted into amide compounds by chemical transformation. MTT method was applied to evaluate their anti-cancer potency. The binding affinity to related proteins was calculated by molecular docking. Results: Totally, 45 new amido-derivatives were synthesized and structurally characterized by NMR and HRMS. Some of them showed moderate to good antiproliferative potency against cancer cells. The activity of compound 10j was further testified by colony formation assay and molecular docking. Conclusion: Synthesis of 23-iodo silybin, 23-iodo hydnocarpin D and 23-iodo isosilandrin from silybin was successfully accomplished by one simple iodination reaction. Some of the amide derivatives of sylibin/hydnocarpin D /silandrin exhibit a remarkable inhibitory effect of proliferation on cancer cells as compared to silybin. These results would pave the way for further investigation on the derivatives of flavonolignans for the treatment of cancer.


2014 ◽  
Vol 82 ◽  
pp. 255-262 ◽  
Author(s):  
Jabeena Khazir ◽  
Irfan Hyder ◽  
J. Laxmi Gayatri ◽  
Leela Prasad Yandrati ◽  
Naresh Nalla ◽  
...  

2013 ◽  
Vol 9 (7) ◽  
pp. 920-925 ◽  
Author(s):  
Yi Bi ◽  
Jinyi Xu ◽  
Fei Sun ◽  
Xiaoming Wu ◽  
Wencai Ye ◽  
...  

Author(s):  
Vasil Tsanov ◽  
Hristo Tsanov

Background:: This article concentrates on the processes occurring in the medium around the cancer cell and the transfer of glycoside amides through their cell membrane. They are obtained by modification of natural glycoside-nitriles (cyano-glycosides). Hydrolysis of starting materials in the blood medium and associated volume around physiologically active healthy and cancer cells, based on quantum-chemical semi-empirical methods, is considered. Objective:: Based on the fact that the cancer cell feeds primarily on carbohydrates, it is likely that organisms have adapted to take food containing nitrile glycosides and / or modified forms to counteract "external" bioactive activity. Cancers, for their part, have evolved to create conditions around their cells that eliminate their active apoptotic forms. This is far more appropriate for them than changing their entire enzyme regulation to counteract it. In this way, it protects itself and the gene sets and develops according to its instructions. Methods:: Derived pedestal that closely defines the processes of hydrolysis in the blood, the transfer of a specific molecular hydrolytic form to the cancer cell membrane and with the help of time-dependent density-functional quantum- chemical methods, its passage and the processes of re-hydrolysis within the cell itself, to forms causing chemical apoptosis of the cell - independent of its non-genetic set, which seeks to counteract the process. Results:: Used in oncology it could turn a cancer from a lethal to a chronic disease (such as diabetes). The causative agent and conditions for the development of the disease are not eliminated, but the amount of cancer cells could be kept low for a long time (even a lifetime). Conclusion:: The amide derivatives of nitrile glycosides exhibit anti-cancer activity, the cancer cell probably seeks to displace hydrolysis of these derivatives in a direction that would not pass through its cell membrane and the amide- carboxyl derivatives of nitrile glycosides could deliver extremely toxic compounds within the cancer cell itself and thus block and / or permanently damage its normal physiology.


2019 ◽  
Vol 19 (7) ◽  
pp. 842-874 ◽  
Author(s):  
Harbinder Singh ◽  
Nihar Kinarivala ◽  
Sahil Sharma

We live in a world with complex diseases such as cancer which cannot be cured with one-compound one-target based therapeutic paradigm. This could be due to the involvement of multiple pathogenic mechanisms. One-compound-various-targets stratagem has become a prevailing research topic in anti-cancer drug discovery. The simultaneous interruption of two or more targets has improved the therapeutic efficacy as compared to the specific targeted based therapy. In this review, six types of dual targeting agents along with some interesting strategies used for their design and synthesis are discussed. Their pharmacology with various types of the molecular interactions within their specific targets has also been described. This assemblage will reveal the recent trends and insights in front of the scientific community working in dual inhibitors and help them in designing the next generation of multi-targeted anti-cancer agents.


2019 ◽  
Vol 89 (3) ◽  
pp. 511-516 ◽  
Author(s):  
B. Ravinaik ◽  
D. Ramachandran ◽  
M. V. Basaveswara Rao

ACS Omega ◽  
2021 ◽  
Author(s):  
Qiang Shang ◽  
Xiaobo Zhou ◽  
Ming-Rong Yang ◽  
Jing-Guang Lu ◽  
Yu Pan ◽  
...  

2021 ◽  
pp. 105065
Author(s):  
Yu-Yuan Chen ◽  
Yin-Peng Bai ◽  
Bin Li ◽  
Xiao-Bo Zhao ◽  
Cheng-Jie Yang ◽  
...  

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