Amide Derivatives of Ginkgolide B and Their Inhibitory Effects on PAF-Induced Platelet Aggregation

SummaryInhibition of blood platelet aggregation by brinolase (fibrinolytic enzyme from Aspergillus oryzae) has been demonstrated with human platelets in vitro and with dog platelets in vivo and in vitro, using both ADP and collagen as aggregating stimuli. It is suggested that the optimal inhibitory effects of brinolase occur indirectly through the generation of plasma fibrinogen degradation products, without compromising platelet viability, rather than by direct proteolysis of platelet structures.

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

10.26226/morressier.57d6b2bbd462b8028d88edfe ◽

2016 ◽

Author(s):

Venumadhav Janganati

Keyword(s):

Design And Synthesis ◽

Amide Derivatives ◽

Anti Cancer ◽

Derivatives Of

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Synthesis and Biological Activity of 28-Amide Derivatives of 23-Hydroxy Betulinic Acid as Antitumor Agent Candidates

Medicinal Chemistry ◽

10.2174/1573406411309070005 ◽

2013 ◽

Vol 9 (7) ◽

pp. 920-925 ◽

Cited By ~ 6

Author(s):

Yi Bi ◽

Jinyi Xu ◽

Fei Sun ◽

Xiaoming Wu ◽

Wencai Ye ◽

...

Keyword(s):

Biological Activity ◽

Betulinic Acid ◽

Antitumor Agent ◽

Amide Derivatives ◽

Derivatives Of

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Theoretical Study of the Process of Passage of Glycoside Amides through the Cell Membrane of Cancer Cell

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520620999201103201008 ◽

2020 ◽

Vol 20 ◽

Author(s):

Vasil Tsanov ◽

Hristo Tsanov

Keyword(s):

Cell Membrane ◽

Cancer Cells ◽

Cancer Cell ◽

Quantum Chemical ◽

Density Functional ◽

Enzyme Regulation ◽

Amide Derivatives ◽

Pass Through ◽

Hydrolysis Of ◽

Derivatives Of

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.

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ChemInform Abstract: THIO AMIDE DERIVATIVES OF 1,2,3-TRIOXOINDAN

Chemischer Informationsdienst ◽

10.1002/chin.197816162 ◽

1978 ◽

Vol 9 (16) ◽

Author(s):

D. MATHIES ◽

K. HAIN

Keyword(s):

Amide Derivatives ◽

Derivatives Of

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Growth Inhibitory Effects of Ester Derivatives of Menahydroquinone-4, the Reduced Form of Vitamin K2(20), on All-Trans Retinoic Acid-Resistant HL60 Cell Line

Pharmaceutics ◽

10.3390/pharmaceutics13050758 ◽

2021 ◽

Vol 13 (5) ◽

pp. 758

Author(s):

Hirofumi Yamakawa ◽

Shuichi Setoguchi ◽

Shotaro Goto ◽

Daisuke Watase ◽

Kazuki Terada ◽

...

Keyword(s):

Retinoic Acid ◽

Adverse Effects ◽

Vitamin K2 ◽

Reduced Form ◽

Inhibitory Effects ◽

Hl60 Cells ◽

Trans Retinoic Acid ◽

All Trans Retinoic Acid ◽

Growth Inhibitory ◽

Derivatives Of

The first-choice drug for acute promyelocytic leukemia (APL), all-trans retinoic acid (ATRA), frequently causes drug-resistance and some adverse effects. Thus, an effective and safe agent for ATRA-resistant APL is needed. Menaquinone-4 (MK-4, vitamin K2(20)), used for osteoporosis treatment, does not have serious adverse effects. It has been reported that MK-4 has growth-inhibitory effects on HL60 cells by inducing apoptosis via the activation of Bcl-2 antagonist killer 1 (BAK). However, the effect of MK-4 on ATRA-resistant APL has not been reported. Here, we show that ester derivatives of menahydroquinone-4 (MKH; a reduced form of MK-4), MKH 1,4-bis-N,N-dimethylglycinate (MKH-DMG) and MKH 1,4-bis-hemi-succinate (MKH-SUC), exerted strong growth-inhibitory effects even on ATRA-resistant HL60 (HL-60R) cells compared with ATRA and MK-4. MKH delivery after MKH-SUC treatment was higher than that after MK-4 treatment, and the results indicated apoptosis induced by BAK activation. In contrast, for MKH-DMG, reconversion to MKH was slow and apoptosis was not observed. We suggest that the ester forms, including monoesters of MKH-DMG, exhibit another mechanism independent of apoptosis. In conclusion, the MKH derivatives (MKH-SUC and MKH-DMG) inhibited not only HL60 cells but also HL-60R cells, indicating a potential to overcome ATRA resistance.

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