scholarly journals Chemical synthesis of dolichyl phosphates, their analogues and derivatives and application of these compounds in biochemical assays.

2007 ◽  
Vol 54 (4) ◽  
pp. 695-701 ◽  
Author(s):  
Leonid L Danilov ◽  
Tatyana N Druzhinina
Keyword(s):  
Chemical Synthesis ◽  
Chemical Modification ◽  
Phosphoryl Group ◽  
Isoprene Unit ◽  
Biochemical Assays

Several methods for simple and efficient chemical synthesis of dolichyl phosphates and their analogues and derivatives are briefly summarized with a special emphasis on chemical modification of phosphoryl group and preparation of dolichyl phosphates labelled at the omega-end and at the gamma-isoprene unit of the isoprene chain by fluorescent groups, 2-aminopyridine and 1-aminonaphtalene residues. Additionally, data on biochemical assays with application of the compounds mentioned above are presented.

Aryltetralin-type lignan of Podophyllum: a comprehensive review

2021 ◽  
Vol 11 ◽  
Author(s):  
Dharmendra Kumar ◽  
Mogana Rajagopal ◽  
Gabriel Akyirem Akowuah ◽  
Yong-Xin Lee ◽  
Chua Wei Chong ◽  
...  
Keyword(s):  
Combination Therapy ◽  
Chemical Synthesis ◽  
Chemical Modification ◽  
Broad Spectrum ◽  
Anticancer Agent ◽  
Review Article ◽  
Pharmacological Activities ◽  
Comprehensive Review ◽  
Podophyllotoxin Derivatives

: Podophyllotoxin is a nonalkaloidtoxin aryltetralin lactone lignan, occurring naturally and extracted from the rhizomes and roots of Podophyllum species. Podophyllotoxin and its derivatives have shown to possess a broad spectrum of pharmacological activities, mainly antineoplastic and antiviral properties. Podophyllotoxin is served as a potential anticancer agent and also the precursor for the chemical synthesis of some clinically important anticancer agents.The chemical modification and pharmacological investigation of podophyllotoxin derivatives have become a concern nowadays. Research interest has been stimulated in the innovation of podophyllotoxin derivatives as the semi-synthetic anticancer agent, especially etoposide and teniposide. Podophyllotoxin and its derivatives are available in several formulations and also found to be effective in combination therapy. This review article aims to provide an overview of the role of podophyllotoxin, its mechanism of action, pharmacological activities, pharmacokinetics, available formulations, and its effects in combination therapy. This article also reviewed the biosynthesis, structure and modifications of podophyllotoxin and its derivatives as an anticancer agent.

The Development of New Low-Molecular-Weight Factor Xa Inhibitors That Are Potential Anticoagulants

2021 ◽  
Vol 18 ◽  
Author(s):  
Dmitry G. Tovbin ◽  
Dmitry N. Tarasov ◽  
Dmitry V. Malakhov ◽  
Natalia A. Tserkovnikova ◽  
Arseniy V. Aybush ◽  
...  
Keyword(s):  
Molecular Weight ◽  
Chemical Synthesis ◽  
Chemical Modification ◽  
Oral Anticoagulants ◽  
Factor Xa ◽  
Activity Measurement ◽  
Low Molecular Weight ◽  
Structure Based Drug Design ◽  
Nanomolar Concentration ◽  
Simple Chemical

Background: Despite the introduction of direct oral anticoagulants, the search for new oral anticoagulants remains an urgent task. Objective: Using the docking and scoring, based on physical methods, simple chemical rules, methods of synthesis and activity measurement, to develop new low-molecular-weight inhibitors of factor Xa, which are potential anticoagulants. Method: The development of leads was based on chemical synthesis and the structure-based drug design methods. The basic idea is to combine the two approaches: one based on predictive modeling, and the other – on the experimental data. Results: In frame of our concept we developed some nanomolar leads. Further chemical modification improved the inhibition constant by more than one order. Discussion: The method proposed in this paper, as well as other methods, includes virtual screening, screening, chemical synthesis and activity measurement. However, the most time – consuming process in this method (chemical synthesis) was decided to simplify and reduce the cost to the extent that it could be allowed: a very simple chemical reaction was chosen - the formation of an amide bond. Conclusion: In this work, we demonstrated how, using simple chemical rules, based on the structure-based drug design, substances with a nanomolar concentration of activity can be developed. Using our method, we developed substances with nanomolar concentration of activity. Further chemical modification of this leads improved the inhibition constant by more than one order.

Chemical synthesis of proteinoids: Part 1

1964 ◽  
Author(s):  
Sidney W. Fox ◽  
Kaoru Harada ◽  
Gottfried Krampitz ◽  
Tadao Hayakawa ◽  
Charles Ray Windsor
Keyword(s):  
Chemical Synthesis

Chemical Synthesis of Peptides

2012 ◽  
Vol 2 (2) ◽  
pp. 147-149
Author(s):  
Tanaji Dnyanadev Padalkar ◽  
Keyword(s):  
Chemical Synthesis
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