Ecdysteroids: isolation, chemical transformations, and biological activity

Phenols are widespread in nature, being the major components of several plants and essential oils. Natural phenols’ anti-microbial, anti-bacterial, anti-oxidant, pharmacological and nutritional properties are, nowadays, well established. Hence, given their peculiar biological role, numerous studies are currently ongoing to overcome their limitations, as well as to enhance their activity. In this review, the functionalization of selected natural phenols is critically examined, mainly highlighting their improved bioactivity after the proper chemical transformations. In particular, functionalization of the most abundant naturally occurring monophenols, diphenols, lipidic phenols, phenolic acids, polyphenols and curcumin derivatives is explored.

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Synthesis and cyclization reactions with pyrazolopyrimidinyl keto esters part I. Reactivity of pyrazolopyrimidinyl β-keto ester and pyrazolopyrimidinyl α,β-unsaturated ketones

Chemical Papers ◽

10.2478/s11696-006-0062-4 ◽

2006 ◽

Vol 60 (5) ◽

Cited By ~ 1

Author(s):

M. Awas

Keyword(s):

Spectral Analysis ◽

Biological Activity ◽

Chemical Transformations ◽

Cyclization Reactions ◽

Keto Ester ◽

Unsaturated Ketones ◽

Keto Esters ◽

Chemical Behaviour ◽

Derivatives Of

Abstract5-Acetyl-4,5-dihydro-1-phenylpyrazolo[3,4-d]pyrimidin-4-one was prepared and subjected to various chemical transformations to give novel 5-heterocyclic pyrazolopyrimidinone derivatives of expected important biological activity. Then, the latter compounds were used to obtain β-keto ester and α,β-unsaturated carbonylpyrazolopyrimidinones which were used as alternate precursors to produce new pyrazolopyrimidinones substituted with five-membered heterocycles such as pyrazole and isoxazole. The structure of these compounds was identified on the basis of their chemical behaviour as well as elemental and spectral analysis.

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SYNTHETIC ROUTES AND NATURAL SOURCES OF 2-PYRIDONE DERIVATIVES AND THEIR PHARMACOLOGICAL ACTIVITY

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2017.v10i7.17989 ◽

2017 ◽

Vol 10 (7) ◽

pp. 87

Author(s):

Vijey Aanandhi M ◽

Ravichandiran V ◽

Prem Shankar Misra

Keyword(s):

Biological Activity ◽

Building Blocks ◽

Medical Application ◽

Heterocyclic Ring ◽

High Reactivity ◽

Molecular Structures ◽

Biologically Active ◽

Natural Occurrence ◽

Chemical Transformations ◽

Substrate Analogs

Objective: 2-pyridone is a well-known heterocyclic ring having significant biological and medical application. The molecular structures and various activities of 2-pyridone derivatives as well as their syntheses and natural occurrence are analyzed and reviewed, and their reactivity toward various nucleophiles is discussed.Methods: 2-pyridone derivatives, first naturally obtained and described as early as before the 19th century, have been attracting increasing attention in view of their high reactivity as building blocks for the preparation of compounds of various classes due to their selective transformations with different reagents. Much information describing the natural occurrence, synthesis and the significant biological activity of 2-pyridone compounds are scattered throughout the literature. There are short chapters dealing with the synthesis and activity of 2-pyridone derivatives.Results: After compiling the above material, the abundance of certain heterocyclic ring and nature of typical chemical transformations applied in current drug synthesis. It is likely this results from the abundance of these heterocycles in natural products such as alkaloids and various synthetic derivatives revealing different biological activity. This might suggest a classical approach to drug design where substrate analogs gain inspiration from existing natural ligands.Conclusions: The data considered in this review clearly demonstrate the high synthetic potential of 2-pyridone derivatives. Many biologically active heterocyclic compounds have been obtained based on this heterocyclic ring. This suggests that 2-pyridone can be used in the design of novel highly effective pharmaceuticals with a broad spectrum of bioresponses.

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Influence of the binding of reduced NAMI-A to human serum albumin on the pharmacokinetics and biological activity

Dalton Transactions ◽

10.1039/c4dt02865a ◽

2015 ◽

Vol 44 (4) ◽

pp. 1905-1913 ◽

Cited By ~ 28

Author(s):

V. Novohradský ◽

A. Bergamo ◽

M. Cocchietto ◽

J. Zajac ◽

V. Brabec ◽

...

Keyword(s):

Biological Activity ◽

Human Serum Albumin ◽

Serum Albumin ◽

Human Serum ◽

Chemical Transformations

Chemical transformations of NAMI-A in biological environments.

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(+)-Larixol and Larixyl Acetate: Syntheses, Phytochemical Studies and Biological Activity Assessments

Chemistry Journal of Moldova ◽

10.19261/cjm.2021.836 ◽

2021 ◽

Author(s):

Alexandru Ciocarlan

Keyword(s):

Biological Activity ◽

Organic Synthesis ◽

Present Review ◽

Phytochemical Analysis ◽

Chemical Transformations ◽

Practical Applications ◽

Phytochemical Studies

(+)-Larixol is a well-known labdane-type diterpenoid widely used in organic synthesis. The present review covers the (+)-larixol based chemical transformations, the results of phytochemical analysis of new (+)-larixol containing species, as well as recent data on biological activity of (+)-larixol and practical applications where it is mentioned.

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A Review on the Chemistry of Eremanthine: A Sesquiterpene Lactone with Relevant Biological Activity

Organic Chemistry International ◽

10.1155/2011/170196 ◽

2011 ◽

Vol 2011 ◽

pp. 1-35 ◽

Cited By ~ 2

Author(s):

José C. F. Alves

Keyword(s):

Biological Activity ◽

Sesquiterpene Lactone ◽

Sesquiterpene Lactones ◽

Chemical Transformations ◽

Structural Classification ◽

Natural Sources

The several aspects on the chemistry of eremanthine such as isolation, structural classification, biological activity, synthesis, and chemical transformations in other sesquiterpene lactones are described in this review. The main publications on this sesquiterpenolide, from its isolation of natural sources in 1972 to the current days, are included.

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

Proceedings, annual meeting, Electron Microscopy Society of America ◽

10.1017/s0424820100072332 ◽

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.

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Effects of Vincristine on Endothelial Microtubules in the Spinal Cord

Proceedings, annual meeting, Electron Microscopy Society of America ◽

10.1017/s0424820100090270 ◽

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.

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