Thrombin inhibitors. 3. Carboxyl-containing amide derivatives of N.alpha.-substituted L-arginine

1980 ◽  
Vol 23 (12) ◽  
pp. 1293-1299 ◽  
Author(s):  
Ryoji Kikumoto ◽  
Yoshikuni Tamao ◽  
Kazuo Ohkubo ◽  
Tohru Tezuka ◽  
Shinji Tonomura ◽  
...  
1981 ◽  
Vol 12 (16) ◽  
Author(s):  
R. KIKUMOTO ◽  
Y. TAMAO ◽  
K. OHKUBO ◽  
T. TEZUKA ◽  
S. TONOMURA ◽  
...  

2006 ◽  
Vol 514-516 ◽  
pp. 961-965 ◽  
Author(s):  
Claudio Salvagnini ◽  
Jacqueline Marchand-Brynaert

Piperazinyl-amide derivatives of N--(3-trifluoromethyl-benzenesulfonyl)-L-arginine were synthesized as graftable thrombin inhibitors. Their biological activity was evaluated in vitro, against human -thrombin, and in blood coagulation assay. The piperazinyl-amide derivatives were found to inhibit the activity of -thrombin in the micromolar range. The designed molecules were fixed on poly(ethylene terephthalate) (PET), and poly(butylene terephthalate) (PBT) by wet chemistry treatment (activation of hydroxyl chain-ends) and photochemistry (nitrene insertion by photoactivation of aromatic azide). The protocols were validated by X-ray photoelectron spectroscopy (XPS) and by radiochemical assay (liquid scintillation counting, LSC).


1981 ◽  
Vol 12 (5) ◽  
Author(s):  
R. KIKUMOTO ◽  
Y. TAMAO ◽  
K. OHKUBO ◽  
T. TEZUKA ◽  
S. TONOMURA ◽  
...  

1980 ◽  
Vol 23 (8) ◽  
pp. 830-836 ◽  
Author(s):  
Ryoji Kikumoto ◽  
Yoshikuni Tamao ◽  
Kazuo Ohkubo ◽  
Tohru Tezuka ◽  
Shinji Tonomura ◽  
...  

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.


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

1984 ◽  
Vol 15 (37) ◽  
Author(s):  
V. P. PEREVALOV ◽  
M. A. ANDREEVA ◽  
YU. A. MANAEV ◽  
SH. G. ISAEV ◽  
L. I. BARYSHNENKOVA ◽  
...  

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