scholarly journals Studying the effect of structural modification of porphyrin derivatives on tumor uptake: Is lipophilicity the sole criterion?

2021 ◽  
Vol 96-97 ◽  
pp. S45-S46
Author(s):  
Mohini Guleria ◽  
Jeyachitra Amirdhanayagam ◽  
Shishu Suman ◽  
Jyotsna Bhatt Mitra ◽  
Sandeep Shelar ◽  
...  
Keyword(s):  
Structural Modification ◽  
Tumor Uptake ◽  
Porphyrin Derivatives ◽  
Sole Criterion

Cristal-growth dynamics of n-doped gaAs

1992 ◽  
Vol 50 (2) ◽  
pp. 1544-1545
Author(s):  
Pham V. Huong ◽  
Stéphanie Bouchet ◽  
Jean-Claude Launay
Keyword(s):  
Crystal Growth ◽  
Spatial Resolution ◽  
Epitaxial Layer ◽  
Outer Surface ◽  
Gaas Substrate ◽  
Structural Modification ◽  
Growth Dynamics ◽  
Argon Laser ◽  
High Anisotropy ◽  
Crystal Gaas

Microstructure of epitaxial layers of doped GaAs and its crystal growth dynamics on single crystal GaAs substrate were studied by Raman microspectroscopy with a Dilor OMARS instrument equipped with a 1024 photodiode multichannel detector and a ion-argon laser Spectra-Physics emitting at 514.5 nm.The spatial resolution of this technique, less than 1 μm2, allows the recording of Raman spectra at several spots in function of thickness, from the substrate to the outer deposit, including areas around the interface (Fig.l).The high anisotropy of the LO and TO Raman bands is indicative of the orientation of the epitaxial layer as well as of the structural modification in the deposit and in the substrate at the interface.With Sn doped, the epitaxial layer also presents plasmon in Raman scattering. This fact is already very well known, but we additionally observed that its frequency increases with the thickness of the deposit. For a sample with electron density 1020 cm-3, the plasmon L+ appears at 930 and 790 cm-1 near the outer surface.

10-step Synthesis of 20-nor-Salvinorin A by Dynamic Strategic Bond Analysis

2017 ◽  
Author(s):  
Jeremy Roach ◽  
Yusuke Sasano ◽  
Cullen Schmid ◽  
Saheem Zaidi ◽  
Vsevolod Katritch ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Opioid Receptors ◽  
Structural Modification ◽  
High Selectivity ◽  
Therapeutic Potential ◽  
Salvinorin A ◽  
High Affinity ◽  
Plant Metabolite ◽  
Complex Architecture ◽  
Property Modification

Salvinorin A (SalA) is a plant metabolite that agonizes the human <i>kappa</i>-opioid receptor (κ-OR) with high affinity and high selectivity over <i>mu- </i>and <i>delta-</i>opioid receptors. Its therapeutic potential has stimulated extensive semi-synthetic studies and total synthesis campaigns. However, structural modification of SalA has been complicated by its instability, and efficient total synthesis has been frustrated by its dense, complex architecture. Treatment of strategic bonds in SalA as dynamic and dependent on structural perturbation enabled the identification of an efficient retrosynthetic pathway. Here we show that deletion of C20 simultaneously stabilizes the SalA skeleton, simplifies its synthesis and retains its high affinity and selectivity for the κ-OR. The resulting 10-step synthesis now opens the SalA scaffold to deep-seated property modification.

Antineoplastic Activity, Structural Modification, Synthesis and Structure-activity Relationship of Dammarane-type Ginsenosides: An Overview

2019 ◽  
Vol 23 (5) ◽  
pp. 503-516 ◽  
Author(s):  
Qiang Zhang ◽  
Xude Wang ◽  
Liyan Lv ◽  
Guangyue Su ◽  
Yuqing Zhao
Keyword(s):  
Structural Modification ◽  
Gastrointestinal Disease ◽  
Structure Activity Relationship ◽  
Cerebrovascular Diseases ◽  
Activity Relationship ◽  
Cycle Arrest ◽  
Structure Activity ◽  
Wide Range ◽  
Structural Association ◽  
Relationship Of

Dammarane-type ginsenosides are a class of tetracyclic triterpenoids with the same dammarane skeleton. These compounds have a wide range of pharmaceutical applications for neoplasms, diabetes mellitus and other metabolic syndromes, hyperlipidemia, cardiovascular and cerebrovascular diseases, aging, neurodegenerative disease, bone disease, liver disease, kidney disease, gastrointestinal disease and other conditions. In order to develop new antineoplastic drugs, it is necessary to improve the bioactivity, solubility and bioavailability, and illuminate the mechanism of action of these compounds. A large number of ginsenosides and their derivatives have been separated from certain herbs or synthesized, and tested in various experiments, such as anti-proliferation, induction of apoptosis, cell cycle arrest and cancer-involved signaling pathways. In this review, we have summarized the progress in structural modification, shed light on the structure-activity relationship (SAR), and offered insights into biosynthesis-structural association. This review is expected to provide a preliminary guide for the modification and synthesis of ginsenosides.

Combinatorial Synthesis of Novel 9R-Acyloxyquinine Derivatives as Insecticidal Agents

2020 ◽  
Vol 23 (2) ◽  
pp. 111-118
Author(s):  
Zhiping Che ◽  
Jinming Yang ◽  
Di Sun ◽  
Yuee Tian ◽  
Shengming Liu ◽  
...  
Keyword(s):  
Natural Products ◽  
Double Bond ◽  
Insecticidal Activity ◽  
Structural Modification ◽  
Combinatorial Synthesis ◽  
Hydroxyl Group ◽  
Botanical Insecticide ◽  
Mythimna Separata ◽  
Lead Compounds

Background: It is one of the effective ways for pesticide innovation to develop new insecticides from natural products as lead compounds. Quinine, the main alkaloid in the bark of cinchona tree as well as in plants in the same genus, is recognized as a safe and potent botanical insecticide to many insects. The structural modification of quinine into 9R-acyloxyquinine derivatives is a potential approach for the development of novel insecticides, which showed more toxicity than quinine. However, there are no reports on the insecticidal activity of 9Racyloxyquinine derivatives to control Mythimna separata. Methods: Endeavor to discover biorational natural products-based insecticides, 20 novel 9Racyloxyquinine derivatives were prepared and assessed for their insecticidal activity against M. separata in vivo by the leaf-dipping method at 1 mg/mL. Results: Among all the compounds, especially derivatives 5i, 5k and 5t exhibited the best insecticidal activity with final mortality rates of 50.0%, 57.1%, and 53.6%, respectively. Conclusion: Overall, a free 9-hydroxyl group is not a prerequisite for insecticidal activity and C9- substitution is well tolerated; modification of out-ring double-bond is acceptable, and hydrogenation of double-bond enhances insecticidal activity; Quinine ring is essential and open of it is not acceptable. These preliminary results will pave the way for further modification of quinine in the development of potential new insecticides.

A Brief Introduction to Porphyrin Compounds Used in Tumor Imaging and Therapies

2020 ◽  
Vol 20 ◽  
Author(s):  
Lili Pan ◽  
Yu Ma ◽  
Xiaoai Wu ◽  
Huawei Cai ◽  
Feng Qin ◽  
...  
Keyword(s):  
Tumor Imaging ◽  
Photoacoustic Imaging ◽  
Therapeutic Agents ◽  
Biochemical Properties ◽  
Therapeutic Effects ◽  
Future Prospects ◽  
Animal Tissues ◽  
Sonodynamic Therapy ◽  
Porphyrin Derivatives ◽  
Porphyrin Analogues

Abstract:: As a group of heterocyclic macrocycle organic natural compounds occurring universally in animal tissues and plants, porphyrins are composed of four modified pyrrole subunits. Porphyrin analogues/derivatives possess multiple biochemical properties because of their unique structures and have been extensively investigated in cancer treatment. Studies have shown that porphyrins and their derivatives have the ability to locate in tumor cells in a variety of human cancers, and these compounds not only exhibit potent therapeutic effects as photodynamic agents but also show promising properties in medicinal imaging, such as MRI, photoacoustic imaging, fluorescence imaging and PET/SPECT imaging. This paper reviews the recent reports of porphyrin derivatives as therapeutic agents used in tumor therapies, such as sonodynamic therapy, photodynamic therapy and radiotherapy, as well as imaging agents for multimodality tumor imaging. The limitations of porphyrin-based compounds in tumor treatments and future prospects are also summarized.

Exploring the Chemistry and Therapeutic Potential of Triazoles: A Comprehensive Literature Review

2019 ◽  
Vol 19 (16) ◽  
pp. 1298-1368 ◽  
Author(s):  
Ankit Jain ◽  
Poonam Piplani
Keyword(s):  
Oxidative Stress ◽  
Drug Discovery ◽  
Literature Review ◽  
Structural Modification ◽  
Therapeutic Potential ◽  
Pharmacological Properties ◽  
Pharmacological Activities ◽  
Triazole Derivatives ◽  
Comprehensive Literature Review ◽  
The Common

: Triazole is a valuable platform in medicinal chemistry, possessing assorted pharmacological properties, which could play a major role in the common mechanisms associated with various disorders like cancer, infections, inflammation, convulsions, oxidative stress and neurodegeneration. Structural modification of this scaffold could be helpful in the generation of new therapeutically useful agents. Although research endeavors are moving towards the growth of synthetic analogs of triazole, there is still a lot of scope to achieve drug discovery break-through in this area. Upcoming therapeutic prospective of this moiety has captured the attention of medicinal chemists to synthesize novel triazole derivatives. The authors amalgamated the chemistry, synthetic strategies and detailed pharmacological activities of the triazole nucleus in the present review. Information regarding the marketed triazole derivatives has also been incorporated. The objective of the review is to provide insights to designing and synthesizing novel triazole derivatives with advanced and unexplored pharmacological implications.

Strategies for Development of Antimalarials Based on Encapsulated Porphyrin Derivatives

2015 ◽  
Vol 14 (13) ◽  
pp. 1055-1071 ◽  
Author(s):  
Daiana Deda ◽  
Alexandre Budu ◽  
Laura Cruz ◽  
Koiti Araki ◽  
Celia Garcia
Keyword(s):  
Porphyrin Derivatives
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