A practical synthetic route to Artepillin C and Drupanin

2021 ◽  
Author(s):  
Xuezheng Zhao ◽  
Lu Wang ◽  
Xiaoya Li ◽  
Qingqing Zhang ◽  
Wei Li ◽  
...  
Keyword(s):  
Synthetic Route ◽  
Artepillin C

A General Convergent Strategy for the Synthesis of Tetrasubstituted Furan Fatty Acids (FuFAs)

2019 ◽  
Author(s):  
Yamin Wang ◽  
Gareth Pritchard ◽  
Marc Kimber
Keyword(s):  
Fatty Acids ◽  
Spectral Data ◽  
Synthetic Route ◽  
Furan Fatty Acids

Synthetic route for the synthesis of tetrasubstituted furan fatty acids; including experimental details, characterisation, and spectral data of all intermediates.

Palladium-Catalyzed Asymmetric Annulation Between Aryl Iodides and Racemic Epoxides Using a Chiral Norbornene Cocatalyst

2018 ◽  
Author(s):  
Guangbin Dong ◽  
Renhe Li
Keyword(s):  
Isopropyl Ester ◽  
Synthetic Route ◽  
Initial Development ◽  
Aryl Iodides ◽  
Palladium Catalyzed

Herein, we describe our initial development of an asymmetric Pd-catalyzed annulation between aryl iodides and racemic epoxides for synthesis of 2,3-dihydrobenzofurans using a chiral norbornene cocatalyst. A series of enantiopure ester-, amide- and imide-substituted norbornenes have been prepared with a reliable synthetic route. Promising enantioselectivity (42-45% ee) has been observed using the isopropyl ester-substituted norbornene (N1*) and the amide-substituted norbornene (N7*).

Synthesis and Biological Properties of some New Lead Sulphonamide and Carboxamide Scaffolds Bearing Coumarin Moiety (Mini Review)

2020 ◽  
Vol 20 ◽  
Author(s):  
Cosmas Chinweike Eze ◽  
Mercy Amarachukwu Ezeokonkwo ◽  
Benjamin Ebere Ezema ◽  
Abraham Efeturi Onoabedje ◽  
David Izuchukwu Ugwu
Keyword(s):  
Biological Properties ◽  
Therapeutic Agents ◽  
Amide Group ◽  
Pharmacological Properties ◽  
Important Class ◽  
Synthetic Route ◽  
Therapeutic Activities

: Coumarin, sulphonamide and amide scaffolds exhibit diverse pharmacological features and constitute an important class of therapeutic agents. In this review, we have discussed the synthesis, biological properties, and SAR of coumarins containing sulphonamide or amide group in the last seven years. Many reviews on the therapeutic activities of coumarins, sulphonamides, and amides have been published, hence the authors focused on coumarin-linked sulphonamide or amide scaffolds. The review provides information on the synthetic route to new coumarins containing sulphonamide or amide groups with improved pharmacological properties.

Potentials of Diphenyl Ether Scaffold as a Therapeutic Agent: A Review

2019 ◽  
Vol 19 (17) ◽  
pp. 1392-1406
Author(s):  
Suvarna G. Kini ◽  
Ekta Rathi ◽  
Avinash Kumar ◽  
Varadaraj Bhat
Keyword(s):  
Therapeutic Agent ◽  
Diphenyl Ether ◽  
Biological Properties ◽  
Industrial Applications ◽  
Synthetic Route ◽  
Structure Activity ◽  
Diphenyl Ethers ◽  
Antiviral Activities ◽  
Synthetic Routes ◽  
The 19Th Century

Diphenyl ethers (DPE) and its analogs have exhibited excellent potential for therapeutic and industrial applications. Since the 19th century, intensive research is perpetuating on the synthetic routes and biological properties of DPEs. Few well-known DPEs are Nimesulide, Fenclofenac, Triclosan, Sorafenib, MK-4965, and MK-1439 which have shown the potential of this moiety as a lead scaffold for different pharmacological properties. In this review, we recapitulate the diverse synthetic route of DPE moiety inclusive of merits and demerits over the classical synthetic route and how this moiety sparked an interest in researchers to discern the SAR (Structure Activity Relationship) for the development of diversified biological properties of DPEs such as antimicrobial, antifungal, antiinflammatory & antiviral activities.

A New Synthetic Route to Acylnitroso Intermediates and Their Applications in HDA and Ene Reactions

2018 ◽  
Vol 15 (3) ◽  
Author(s):  
Ahmad Fakhruddin ◽  
Abdel-Moneim Abu-Elfotoh ◽  
Kazutaka Shibatomi ◽  
Seiji Iwasa
Keyword(s):  
Synthetic Route ◽  
Ene Reactions

Artepillin C Induces Selective Oxidative Stress and Inhibits Migration and Invasion in a Comprehensive Panel of Human Cervical Cancer Cell Lines

2019 ◽  
Vol 18 (12) ◽  
pp. 1750-1760 ◽  
Author(s):  
Raquel P. Souza ◽  
Patrícia S. Bonfim-Mendonça ◽  
Gabrielle M.Z.F. Damke ◽  
Analine R.B. de-Assis Carvalho ◽  
Bianca A. Ratti ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Cervical Cancer ◽  
Cell Lines ◽  
Migration And Invasion ◽  
Epithelial Cell Line ◽  
Cellular Viability ◽  
Hpv 16 ◽  
Anticancer Properties ◽  
Artepillin C ◽  
Human Cervical Cancer

Background: Artepillin C (3,5-diprenyl-4-hydroxycinnamic acid) is the main bioactive component of Brazilian green propolis, and possesses, among other things, anticancer properties. However, to the best of our knowledge, there are no studies of artepillin C in cervical cancer. Method: To explore a new therapeutic candidate for cervical cancer, we have evaluated the effects of artepillin C on cellular viability in a comprehensive panel of human cervical cancer-derived cell lines including HeLa (human papillomavirus/HPV 18-positive), SiHa (HPV 16-positive), CaSki (HPV 16- and 18-positive) and C33A (HPV-negative) cells compared to a spontaneously immortalized human epithelial cell line (HaCaT). Results: Our results demonstrated that artepillin C had a selective effect on cellular viability and could induce apoptosis possibly by intrinsic pathway, likely a result of oxidative stress, in all cancer-derived cell lines but not in HaCaT. Additionally, artepillin C was able to inhibit the migration and invasion of cancer cells. Conclusion: Thus, artepillin C appears to be a promising new candidate as an anticancer drug for cervical cancer induced by different HPV types.

A synthetic route to 2,6-bis-triazolyl purine deoxynucleosides via click chemistry

2014 ◽  
Author(s):  
Dace Cīrule ◽  
Kristers Ozols ◽  
Irina Novosjolova ◽  
Māris Turks ◽  
Ērika Bizdēna
Keyword(s):  
Click Chemistry ◽  
Synthetic Route
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