Synthesis of demethoxycapillarisin, a naturally occurring 2-phenoxychromone, and related compounds

Author(s):  
Hidekazu Takeno ◽  
Masashi Hashimoto ◽  
Yoshiyasu Koma ◽  
Haruo Horiai ◽  
Hiroyuki Kikuchi
Biomolecules ◽  
2021 ◽  
Vol 11 (4) ◽  
pp. 603
Author(s):  
Zinnia Shah ◽  
Umar Farooq Gohar ◽  
Iffat Jamshed ◽  
Aamir Mushtaq ◽  
Hamid Mukhtar ◽  
...  

Podophyllotoxin, along with its various derivatives and congeners are widely recognized as broad-spectrum pharmacologically active compounds. Etoposide, for instance, is the frontline chemotherapeutic drug used against various cancers due to its superior anticancer activity. It has recently been redeveloped for the purpose of treating cytokine storm in COVID-19 patients. Podophyllotoxin and its naturally occurring congeners have low bioavailability and almost all these initially discovered compounds cause systemic toxicity and development of drug resistance. Moreover, the production of synthetic derivatives that could suffice for the clinical limitations of these naturally occurring compounds is not economically feasible. These challenges demanded continuous devotions towards improving the druggability of these drugs and continue to seek structure-optimization strategies. The discovery of renewable sources including microbial origin for podophyllotoxin is another possible approach. This review focuses on the exigency of innovation and research required in the global R&D and pharmaceutical industry for podophyllotoxin and related compounds based on recent scientific findings and market predictions.


2018 ◽  
Vol 55 (3) ◽  
pp. 666-672 ◽  
Author(s):  
John F Anderson ◽  
Francis J Ferrandino ◽  
Michael P Vasil ◽  
Robert H Bedoukian ◽  
Marie Maher ◽  
...  

1981 ◽  
Vol 12 (40) ◽  
Author(s):  
H. TAKENO ◽  
M. HASHIMOTO ◽  
Y. KOMA ◽  
H. HORIAI ◽  
H. KIKUCHI

2017 ◽  
Vol 12 (2) ◽  
pp. 1934578X1701200 ◽  
Author(s):  
Daniela Hulcová ◽  
Kateřina Breiterová ◽  
Lucie Zemanová ◽  
Tomáš Siatka ◽  
Marcela Šafratová ◽  
...  

Aldo-keto reductase 1C3 (AKR1C3) is an important human enzyme that participates in the reduction of steroids and prostaglandins, which leads to proliferative signaling. AKR1C3 is frequently upregulated in various cancers, and this enzyme has been suggested as a therapeutic target for the treatment of these pathological conditions. The fact that the isoquinoline alkaloid stylopine has been identified as a potent AKR1C3 inhibitor has prompted us to screen a library of diverse types of Amaryllidaceae alkaloids, which biogenetically are isoquinoline alkaloids, on a recombinant form of AKR1C3. From the tested compounds, only tazettine showed moderate AKR1C3 inhibitory potency with an IC50 value of 15.8 ± 1.2 μM. Tazettine is a common Amaryllidaceae alkaloid, which could be used as a model substance for the further development of either analogues or related compounds with better inhibition potency.


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