Synthesis and biological activity of certain 6-substituted and 2,6-disubstituted 2'-deoxytubercidins prepared via the stereospecific sodium salt glycosylation procedure

1985 ◽  
Vol 28 (10) ◽  
pp. 1461-1467 ◽  
Author(s):  
Howard B. Cottam ◽  
Zygmunt Kazimierczuk ◽  
Stewart Geary ◽  
Patricia A. McKernan ◽  
Ganapathi R. Revankar ◽  
...  
Keyword(s):  
Biological Activity ◽  
Sodium Salt

[5-(Adenin-9-yl)-5-deoxypentofuranosyl]phosphonates - A Novel Type of Nucleotide Analogs Related to HPMPA. I. Derivatives with L-arabino, D-arabino, 2-Deoxy-L-erythro and 2-Deoxy-L-threo Configuration

1993 ◽  
Vol 58 (9) ◽  
pp. 2159-2179 ◽  
Author(s):  
Miroslav Otmar ◽  
Ivan Rosenberg ◽  
Milena Masojídková ◽  
Antonín Holý
Keyword(s):  
Biological Activity ◽  
Sodium Salt ◽  
Triethyl Phosphite ◽  
Membered Ring ◽  
Total Loss ◽  
Arbuzov Reaction ◽  
Partial Structure ◽  
Nucleotide Analogs ◽  
New Type

[5-(Adenin-9-yl)-5-deoxypentofuranosyl]phosphonates, a new type of nucleotide analogs with fixed HPMPA structure, have been prepared. The synthesis of compounds of L-arabino (IIa, IIb), D-arabino(XIVa, XIVb), 2-deoxy-L-erythro(IIIa, IIIb) and 2-deoxy-L-threo(IVa, IVb) configuration is based on the Michelis-Arbuzov reaction of the fully protected methyl glycosides with triethyl phosphite and trimethylsilyl triflate which leads to anomeric mixture of diethyl (L-pentofuranosyl) phosphonates. The protected 5-O-tosyl derivatives react with sodium salt of adenine to give N9-substituted products which after total deprotection afforded the tittle nucleotide analogs. The fixation of the partial structure of HPMPA to form five-membered ring leads to a significant decrease, or a total loss, of biological activity.

Design and Synthesis of Phosphonoacetic Acid (PPA) Ester and Amide Bioisosters of Ribofuranosylnucleoside Diphosphates as Potential Ribonucleotide Reductase Inhibitors and Evaluation of Their Enzyme Inhibitory, Cytostatic and Antiviral Activity

2003 ◽  
Vol 14 (4) ◽  
pp. 183-194 ◽  
Author(s):  
Stefano Manfredini ◽  
Nicola Solaroli ◽  
Angela Angusti ◽  
Federico Nalin ◽  
Elisa Durini ◽  
...  
Keyword(s):  
Biological Activity ◽  
Ribonucleotide Reductase ◽  
Sodium Salt ◽  
Inhibitory Activity ◽  
Acid Amide ◽  
Phosphonoacetic Acid ◽  
Design And Synthesis ◽  
Reductase Inhibitors ◽  
Ribonucleotide Reductase Inhibitors ◽  
Hiv 1

Continuing our investigations on inhibitors of ribonucleotide reductase (RNR), the crucial enzyme that catalyses the reduction of ribonu-cleotides to deoxyribonucleotides, we have now prepared and evaluated 5′-phosphonoacetic acid, amide and ester analogues of adenosine, uridine and cytidine with the aim to verify both substrate specificity and contribution to biological activity of diphosphate mimic moieties. A molecular modelling study has been conducted on the RNR R1 subunit, in order to verify the possible interaction of the proposed bioisosteric moieties. The study compounds were finally tested on the recombinant murine RNR showing a degree of inhibition that ranged from 350 μM for the UDP analogue 5′-deoxy-5′- N-(phosphon-acetyl)uridine sodium salt (amide) to 600 μM for the CDP analogue 5′- O-[(diethyl-phosphon)acetyl]cytidine (ester). None of the tested compounds displayed noteworthy cytostatic activity at 100–500 μM concentrations, whereas ADP analogue 5′- N-[(diethyl-phosphon) acetyl]adenosine (amide) and 5′-deoxy-5′- N-(phos-phon-acetyl)adenosine sodium salt (amide) showed a moderate inhibitory activity (EC50: 48 μM) against HSV-2 and a modest inhibitory activity (EC50: 110 μM) against HIV-1, respectively.

Virus-Like Particles in a Human Breast Cancer: Structural Similarity to Previously Reported Particles

1973 ◽  
Vol 31 ◽  
pp. 378-379
Author(s):  
G. Kasnic ◽  
S. E. Stewart ◽  
C. Urbanski
Keyword(s):  
Breast Cancer ◽  
Biological Activity ◽  
Human Breast Cancer ◽  
Osteogenic Sarcoma ◽  
Human Tumor ◽  
Structural Similarity ◽  
Cell Tumor ◽  
Human Breast ◽  
Human Tumor Cell ◽  
Type Particle

We have reported the maturation of an intracisternal A-type particle in murine plasma cell tumor cultures and three human tumor cell cultures (rhabdomyosarcoma, lung adenocarcinoma, and osteogenic sarcoma) after IUDR-DMSO activation. In all of these studies the A-type particle seems to develop into a form with an electron dense nucleoid, presumably mature, which is also intracisternal. A similar intracisternal A-type particle has been described in leukemic guinea pigs. Although no biological activity has yet been demonstrated for these particles, on morphologic grounds, and by the manner in which they develop within the cell, they may represent members of the same family of viruses.

Effects of Vincristine on Endothelial Microtubules in the Spinal Cord

1976 ◽  
Vol 34 ◽  
pp. 58-59
Author(s):  
John L. Beggs ◽  
John D. Waggener ◽  
Wanda Miller
Keyword(s):  
Spinal Cord ◽  
Biological Activity ◽  
Horseradish Peroxidase ◽  
Transport Mechanism ◽  
Vasogenic Edema ◽  
Vesicular Transport ◽  
Close Proximity

Microtubules (MT) are versatile organelles participating in a wide variety of biological activity. MT involvement in the movement and transport of cytoplasmic components has been well documented. In the course of our study on trauma-induced vasogenic edema in the spinal cord we have concluded that endothelial vesicles contribute to the edema process. Using horseradish peroxidase as a vascular tracer, labeled endothelial vesicles were present in all situations expected if a vesicular transport mechanism was in operation. Frequently,labeled vesicles coalesced to form channels that appeared to traverse the endothelium. The presence of MT in close proximity to labeled vesicles sugg ested that MT may play a role in vesicular activity.

Soft ionic liquid based resistive memory characteristics in a two terminal discrete polydimethylsiloxane cylindrical microchannel

2020 ◽  
Vol 8 (38) ◽  
pp. 13368-13374
Author(s):  
Muhammad Umair Khan ◽  
Gul Hassan ◽  
Jinho Bae
Keyword(s):  
Ionic Liquid ◽  
Acrylic Acid ◽  
Sodium Hydroxide ◽  
Sodium Salt ◽  
Resistive Memory ◽  
Cylindrical Microchannel ◽  
Memory Characteristics ◽  
Poly Acrylic Acid

This paper proposes a novel soft ionic liquid (IL) electrically functional device that displays resistive memory characteristics using poly(acrylic acid) partial sodium salt (PAA-Na+:H2O) solution gel and sodium hydroxide (NaOH) in a thin polydimethylsiloxane (PDMS) cylindrical microchannel.

Isothiazol-3(2 H )-ones, Part I: Synthesis, Reactions and Biological Activity

2002 ◽  
Vol 23 (1) ◽  
pp. 79-121 ◽  
Author(s):  
Kathleen Taubert ◽  
Susanne Kraus ◽  
Bärbel Schulze
Keyword(s):  
Biological Activity ◽  
Synthesis Reactions

Evaluation of biological activity of lignans extracted from tree knots

Planta Medica ◽  
2008 ◽  
Vol 74 (09) ◽  
Author(s):  
E Spilioti ◽  
B Holmbom ◽  
P Moutsatsou
Keyword(s):  
Biological Activity
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