scholarly journals Features of the synthesis and biological evaluation of 3-(carboxyphenyl)chromones

2020 ◽  
Vol 15 (2) ◽  
pp. 3-12
Author(s):  
Olga Shablykina ◽  
Viktoriia Moskvina ◽  
Volodymyr Khilya
Keyword(s):  
Biological Activity ◽  
Biological Evaluation ◽  
Therapeutic Agents ◽  
New Drugs ◽  
Pharmacological Activities ◽  
Chromone Derivatives ◽  
Methods Of Synthesis ◽  
Patent Literature ◽  
Synthetic Routes ◽  
Synthesis And Biological Evaluation

Flavonoids and their derivatives have historically been a source of therapeutic agents. Every year, more and more data is published on new flavonoid compounds, both synthetic and isolated from natural sources, and their innumerable physiological and pharmacological activities. This review presents synthetic routes towards 3-(carboxyphenyl)chromones and evaluation of their biological activity as published in both journal and patent literature. We have focused specifically on the 3-(carboxyphenyl)chromones, because while methods of synthesis and biological activity of 2(3)-substituted and 2,3-disubstituted chromones are well studied, literature data on isoflavones containing a carboxyl, ester, or amide group in ring B is scarce and fragmentary. The presented generalization of synthetic strategies and biological activity of 3-(carboxyphenyl)chromone derivatives demonstrates that this class of compounds can be targeted for discovery of new drugs and can be readily prepared owing to recent advances in synthetic organic and medicinal chemistry.

Synthesis and Biological Evaluation of Various New Substituted 1,3,4-oxadiazole-2-thiols

2008 ◽  
Vol 59 (4) ◽  
Author(s):  
Gabriela Laura Almajan ◽  
Stefania Felicia Barbuceanu ◽  
Ioana Saramet ◽  
Mihaela Dinu ◽  
Cristian Vasile Doicin ◽  
...  
Keyword(s):  
Biological Activity ◽  
Plant Growth ◽  
1H Nmr ◽  
Elemental Analysis ◽  
13C Nmr ◽  
Biological Evaluation ◽  
Ethyl Chloroacetate ◽  
Low Concentrations ◽  
Synthesis And Biological Evaluation

5-[4-(4X-phenylsulfonyl)phenyl]-1,3,4-oxadiazole-2-thiols, X=H, Cl, Br, reacted with ethyl chloroacetate to give S-alkylated compounds. Aminomethylation of the thione form of oxadiazoles yielded N(3)-derivatives. All the products have been characterized by elemental analysis, IR, 1H-NMR and 13C-NMR. The plant-growth regulating effects of the title compounds were examined. From the biological activity results, we found that most compounds showed weak stimulatory activities at low concentrations.

The Synthesis and Biological Evaluation of Anithiactin A/Thiasporine C and Analogues

2015 ◽  
Vol 68 (12) ◽  
pp. 1829 ◽  
Author(s):  
Richard A. Lamb ◽  
Michael P. Badart ◽  
Brooke E. Swaney ◽  
Sinan Gai ◽  
Sarah K. Baird ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Biological Activity ◽  
Cell Lines ◽  
Breast Cancer Cell ◽  
Phenyl Group ◽  
Biological Evaluation ◽  
Breast Cancer Cell Lines ◽  
High Concentration ◽  
Structural Requirements ◽  
Synthesis And Biological Evaluation

The synthesis of anithiactin A has been achieved in four steps. Several closely related analogues were synthesised and their biological activity against colon and breast cancer cell lines evaluated. Anithiactin A was found not to be cytotoxic even at a high concentration (100 μM); however, two 4-substituted phenyl thiazoles were found to be moderately cytotoxic at 10 μM. Based on these results, 4-substitution on the phenyl group appears to be critical for cytotoxicity. However, the exact electronic and structural requirements are unclear.

Phosphate tricyclic coumarin analogs as steroid sulfatase inhibitors: synthesis and biological activity

RSC Advances ◽  
2014 ◽  
Vol 4 (84) ◽  
pp. 44350-44358 ◽  
Author(s):  
Witold Kozak ◽  
Mateusz Daśko ◽  
Maciej Masłyk ◽  
Jerzy S. Pieczykolan ◽  
Bartłomiej Gielniewski ◽  
...  
Keyword(s):  
Biological Activity ◽  
Biological Evaluation ◽  
Steroid Sulfatase ◽  
Coumarin Derivatives ◽  
Synthesis And Biological Evaluation

In the present work, we report convenient methods for the synthesis and biological evaluation of phosphate tricyclic coumarin derivatives as potential steroid sulfatase inhibitors.

scholarly journals Synthesis and Biological Evaluation of N-Heterocyclic Substituted Fluoro-Benzothiazole Sulphonamido Analogs as a Potential Therapeutic Agents

2022 ◽  
Vol 11 (1) ◽  
Author(s):  
Sri Ranga. T ◽  
Neelesh Chaubey
Keyword(s):  
Biological Evaluation ◽  
Therapeutic Agents ◽  
Synthesis And Biological Evaluation

The present investigation is aimed to synthesize fluorobenzothiazole comprising sulphonamido pyrazole analogs starting from fluoro-chloroaniline  to get 2-amino-6-fluoro-7-chloro (1,3) benzothiazole (I), this was treated with anilino-s-methyl ethylene cyanoacetamide  in the presence of ethanol to get desired molecules. The synthesized targeted molecules are characterized, docked and screened  for their invitro antidiabetic properties. Keywords: Fluorobenzothiazole, Docking, antidiabetic

scholarly journals Regorafenib analogues and their ferrocenic counterparts: synthesis and biological evaluation

2020 ◽  
Vol 44 (45) ◽  
pp. 19723-19733
Author(s):  
Myron Wilde ◽  
Danielle Arzur ◽  
Blandine Baratte ◽  
Dorian Lefebvre ◽  
Thomas Robert ◽  
...  
Keyword(s):  
Biological Activity ◽  
Biological Evaluation ◽  
Cellular Assays ◽  
Synthesis And Biological Evaluation

New ferrocene analogues of regorafenib have been prepared and their biological activity was evaluated in kinase and cellular assays.

scholarly journals Novel Synthesis and Biological Evaluation of Enigmols as Therapeutic Agents for Treating Prostate Cancer

2011 ◽  
Vol 2 (6) ◽  
pp. 438-443 ◽  
Author(s):  
Ethel C. Garnier-Amblard ◽  
Suzanne G. Mays ◽  
Richard F. Arrendale ◽  
Mark T. Baillie ◽  
Anatoliy S. Bushnev ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Biological Evaluation ◽  
Therapeutic Agents ◽  
Novel Synthesis ◽  
Synthesis And Biological Evaluation

Synthesis and Biological Evaluation of PF-543 Derivative

2018 ◽  
Vol 16 (1) ◽  
pp. 2-5 ◽  
Author(s):  
Seon Woong Kim ◽  
Taeho Lee ◽  
Joo-Youn Lee ◽  
Sanghee Kim ◽  
Hee-Sook Jun ◽  
...  
Keyword(s):  
Biological Activity ◽  
Structural Information ◽  
Docking Study ◽  
Inhibitory Effect ◽  
Biological Evaluation ◽  
Antineoplastic Activity ◽  
Pc3 Cells ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

PF-543 has been known as a substance that strongly inhibits SK1. However, it also exhibits antineoplastic activity that is lower than other inhibitors of SK1. In this study, we compared PF-543 and synthesized a newly designed derivative of PF-543 (compound 2) in which two aromatic structures were connected in para-form. The synthesized derivative showed inhibitory effect on SK1, similar to that of PF-543. However, it was more cytotoxic to HT29, AGS, and PC3 cells than PF-543. We also carried out a docking study for SK1 and demonstrated that the synthesized derivative showed interaction with SK1 similar to PF-543. Results obtained from this study suggest that the structure of compound 2 may be well substituted for the structure of PF-543 in terms of biological activity, providing us important structural information for the design of new derivatives of PF-543.

Synthesis and biological evaluation of pentacyclo[5.4.0.02,6.03,10.05,9]undecane derivatives as potential therapeutic agents in Parkinson's disease

2004 ◽  
Vol 12 (7) ◽  
pp. 1799-1806 ◽  
Author(s):  
Werner J Geldenhuys ◽  
Sarel F Malan ◽  
Thangaraju Murugesan ◽  
Cornelis J Van der Schyf ◽  
Jeffrey R Bloomquist
Keyword(s):  
Parkinson’S Disease ◽  
Parkinson's Disease ◽  
Biological Evaluation ◽  
Therapeutic Agents ◽  
Synthesis And Biological Evaluation
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