scholarly journals One-pot synthesis, anti-tumor evaluation and structure–activity relationships of novel 25-OCH3-PPD derivatives

MedChemComm ◽  
2017 ◽  
Vol 8 (9) ◽  
pp. 1845-1849 ◽  
Author(s):  
Fan-Zhi Qu ◽  
Chen Zhao ◽  
Jia-Qing Cao ◽  
Yan Zhang ◽  
Yu-Qing Zhao
Keyword(s):  
Panax Ginseng ◽  
Synthetic Method ◽  
Lead Compound ◽  
One Pot ◽  
Structure Activity Relationships ◽  
One Pot Synthesis ◽  
Structure Activity

Based on the fact that 25-OCH3-PPD, a natural ginsengenin isolated from the leaves of Panax ginseng, is a promising lead compound, novel 25-OCH3-PPD derivatives were synthesized to find more potent anti-tumor agents by a simple and facile synthetic method.

A Review on Biological Properties and Synthetic Methodologies of the Diarylpentadienones

2020 ◽  
Vol 20 ◽  
Author(s):  
Maryam Aisyah Abdullah ◽  
Siti Munirah Mohd Faudzi ◽  
Nadiah Mad Nasir
Keyword(s):  
Biological Properties ◽  
Review Article ◽  
High Potential ◽  
One Pot ◽  
One Pot Synthesis ◽  
Structure Activity ◽  
Synthetic Methodologies ◽  
Relationship Of ◽  
Effective Drugs ◽  
Enhanced Stability

Abstract:: Medicinal chemists have continuously shown interest in new curcuminoid derivatives, the diarylpentadienones, owing to their enhanced stability feature and easy preparation using a one-pot synthesis. Thus far, methods such as Claisen-Schmidt condensation and Julia-Kocienski olefination have been utilised for the synthesis of these compounds. Diarylpentadienones possess a high potential as a chemical source for designing and developing new and effective drugs for the treatment of diseases, including inflammation, cancer, and malaria. In brief, this review article focuses on the broad pharmacological applications and the summary of the structure-activity relationship of molecules which can be employed to further explore the structure of diarylpentadienone. The current methodological developments towards the synthesis of diarylpentadienones are also discussed.

scholarly journals Synthesis, Antiprotozoal Activity, and Cheminformatic Analysis of 2-Phenyl-2H-Indazole Derivatives

Molecules ◽  
2021 ◽  
Vol 26 (8) ◽  
pp. 2145
Author(s):  
Karen Rodríguez-Villar ◽  
Lilián Yépez-Mulia ◽  
Miguel Cortés-Gines ◽  
Jacobo David Aguilera-Perdomo ◽  
Edgar A. Quintana-Salazar ◽  
...  
Keyword(s):  
Phenyl Ring ◽  
Medicinal Chemistry ◽  
Structural Features ◽  
Pharmacological Properties ◽  
Antiprotozoal Activity ◽  
One Pot ◽  
Biological Assays ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Synthetic Methodologies

Indazole is an important scaffold in medicinal chemistry. At present, the progress on synthetic methodologies has allowed the preparation of several new indazole derivatives with interesting pharmacological properties. Particularly, the antiprotozoal activity of indazole derivatives have been recently reported. Herein, a series of 22 indazole derivatives was synthesized and studied as antiprotozoals. The 2-phenyl-2H-indazole scaffold was accessed by a one-pot procedure, which includes a combination of ultrasound synthesis under neat conditions as well as Cadogan’s cyclization. Moreover, some compounds were derivatized to have an appropriate set to provide structure-activity relationships (SAR) information. Whereas the antiprotozoal activity of six of these compounds against E. histolytica, G. intestinalis, and T. vaginalis had been previously reported, the activity of the additional 16 compounds was evaluated against these same protozoa. The biological assays revealed structural features that favor the antiprotozoal activity against the three protozoans tested, e.g., electron withdrawing groups at the 2-phenyl ring. It is important to mention that the indazole derivatives possess strong antiprotozoal activity and are also characterized by a continuous SAR.

scholarly journals A rare γ-pyranopyrazole skeleton: design, one-pot synthesis and computational study

2016 ◽  
Vol 14 (31) ◽  
pp. 7490-7494 ◽  
Author(s):  
Muhammed Üçüncü ◽  
Ceren Cantürk ◽  
Erman Karakuş ◽  
Hüseyin Zeybek ◽  
Uğur Bozkaya ◽  
...  
Keyword(s):  
Computational Study ◽  
Synthetic Method ◽  
One Pot ◽  
One Pot Synthesis

A base mediated one-pot, two-step synthetic method for constructing γ-pyranopyrazoles.

A facile one-pot synthesis of deep blue luminescent lead bromide perovskite microdisks

2015 ◽  
Vol 51 (91) ◽  
pp. 16385-16388 ◽  
Author(s):  
Zhao Yuan ◽  
Yu Shu ◽  
Yu Tian ◽  
Yan Xin ◽  
Biwu Ma
Keyword(s):  
Thin Films ◽  
Room Temperature ◽  
Quantum Yields ◽  
Synthetic Method ◽  
Lateral Size ◽  
One Pot ◽  
One Pot Synthesis ◽  
Deep Blue ◽  
Lead Bromide

We report a facile one-pot synthetic method to prepare highly luminescent layered lead(ii) bromide perovskite microdisks with the lateral size of a few micrometers and thickness of 100–150 nm, featuring narrow deep blue emissions with quantum yields of up to 53% in toluene solutions and thin films at room temperature.

scholarly journals One-Pot Synthesis of α-Substituted Acrylates

SynOpen ◽  
2018 ◽  
Vol 02 (02) ◽  
pp. 0161-0167
Author(s):  
Magdalini Matziari ◽  
Yixin Xie
Keyword(s):  
Amino Acids ◽  
Reaction Times ◽  
Synthetic Method ◽  
One Pot ◽  
Biologically Relevant ◽  
Mild Conditions ◽  
One Pot Synthesis ◽  
Acrylic Esters ◽  
Natural Amino Acids ◽  
Work Up

A simple and efficient synthetic method towards α-substituted acrylic esters has been developed using the Horner–Wadsworth–Emmons (HWE) reaction with HCHO after alkylation of phosphonoacetates in a one-pot reaction. This method allows the smooth introduction of various side-chains, such as natural amino acids and other biologically relevant substituents. The use of mild conditions, inexpensive reagents, short reaction times and simple work-up and purification steps provides an effective and general alternative to cumbersome multistep and low-yielding procedures described to date.

scholarly journals One-pot synthesis of substituted pyrrolo[3,4-b]pyridine-4,5-diones based on the reaction of N-(1-(4-hydroxy-6-methyl-2-oxo-2H-pyran-3-yl)-2-oxo-2-arylethyl)acetamide with amines

2019 ◽  
Vol 15 ◽  
pp. 2840-2846
Author(s):  
Valeriya G Melekhina ◽  
Andrey N Komogortsev ◽  
Boris V Lichitsky ◽  
Vitaly S Mityanov ◽  
Artem N Fakhrutdinov ◽  
...  
Keyword(s):  
Starting Material ◽  
Primary Amines ◽  
Synthetic Method ◽  
One Pot ◽  
One Pot Synthesis ◽  
Major Reaction Product ◽  
Major Reaction

The condensation of primary amines with N-(1-(4-hydroxy-6-methyl-2-oxo-2H-pyran-3-yl)-2-oxo-2-arylethyl)acetamides was explored. Thus, a previously unknown recyclization of the starting material was observed in acidic ethanol in the presence of an amine, which provided the corresponding dihydropyrrolone derivative as the major reaction product. Based on this transformation, a practical and convenient one-pot synthetic method for substituted pyrrolo[3,4-b]pyridin-5-ones could be devised.

One-pot synthesis of bi-metallic PdRu tripods as an efficient catalyst for electrocatalytic nitrogen reduction to ammonia

2019 ◽  
Vol 7 (2) ◽  
pp. 801-805 ◽  
Author(s):  
Hongjing Wang ◽  
Yinghao Li ◽  
Chunjie Li ◽  
Kai Deng ◽  
Ziqiang Wang ◽  
...  
Keyword(s):  
Synthetic Method ◽  
One Pot ◽  
Efficient Catalyst ◽  
Nitrogen Reduction ◽  
One Pot Synthesis ◽  
One Step

A very simple one-step synthetic method is developed for fabrication of PdRu tripods for electrochemical nitrogen reduction to ammonia.

Transition-metal-free, one-pot synthesis of Benzoxaboroles from o-bromobenzaldehydes via visible-light-promoted borylation

2021 ◽  
Author(s):  
Jinghan Luo ◽  
Xingxing Jia ◽  
Yanjun Hu ◽  
Jianchao Chen ◽  
Tiemin Sun
Keyword(s):  
Transition Metal ◽  
Visible Light ◽  
Synthetic Method ◽  
One Pot ◽  
Metal Free ◽  
One Pot Synthesis ◽  
Stepwise Method

A novel and simple one-pot stepwise method to synthesize benzoxaboroles was demonstrated. This step-by-step synthetic method includes photocatalytic boronization with phenothiazine as photocatalyst and sequencely water-induced reduction in the presence...

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