Synthesis of α-methylstilbenes using an aqueous Wittig methodology and application toward the development of potent human aromatase inhibitors

2019 ◽  
Vol 29 (11) ◽  
pp. 1395-1398
Author(s):  
Alexander J. Nielsen ◽  
Sergio Raez-Villanueva ◽  
Denis J. Crankshaw ◽  
Alison C. Holloway ◽  
James McNulty
Keyword(s):  
Aromatase Inhibitors ◽  
Human Aromatase

Integrated in silico-in vitro strategy for screening of some traditional Egyptian plants for human aromatase inhibitors

2018 ◽  
Vol 224 ◽  
pp. 359-372 ◽  
Author(s):  
Hend M. Dawood ◽  
Reham S. Ibrahim ◽  
Eman Shawky ◽  
Hala M. Hammoda ◽  
Aly M. Metwally
Keyword(s):  
Aromatase Inhibitors ◽  
In Silico ◽  
Human Aromatase

Computational insights into inhibitory mechanism of azole compounds against human aromatase

RSC Advances ◽  
2015 ◽  
Vol 5 (110) ◽  
pp. 90871-90880 ◽  
Author(s):  
Jinya Cai ◽  
Junhao Li ◽  
Juan Zhang ◽  
Shihui Ding ◽  
Guixia Liu ◽  
...  
Keyword(s):  
Aromatase Inhibitors ◽  
Inhibitory Mechanism ◽  
Human Aromatase

We investigated the inhibitory mechanism of azole aromatase inhibitors. The results showed that letrozole and imazalil prefer different unbinding pathways.

scholarly journals Facile Synthesis of Chrysin-derivatives with Promising Activities as Aromatase Inhibitors†

2011 ◽  
Vol 6 (1) ◽  
pp. 1934578X1100600 ◽  
Author(s):  
Hamdoon A. Mohammed ◽  
Lalla A. Ba ◽  
Torsten Burkholz ◽  
Elena Schumann ◽  
Britta Diesel ◽  
...  
Keyword(s):  
Aromatase Inhibitors ◽  
Anticancer Agents ◽  
Multicomponent Reactions ◽  
Multicomponent Synthesis ◽  
Facile Synthesis ◽  
Functional Elements ◽  
Lead Structure ◽  
New Class ◽  
Flavone Derivatives ◽  
Human Aromatase

Flavones such as chrysin show structural similarities to androgens, the substrates of human aromatase, which converts androgens to estrogens. Aromatase is a key target in the treatment of hormone-dependent tumors, including breast cancer. Flavone-based aromatase inhibitors are of growing interest, and chrysin in particular provides a (natural) lead structure. This paper reports multicomponent synthesis as a means for facile modification of the chrysin core structure in order to add functional elements. A Mannich-type reaction was used to synthesize a range of mono- and disubstituted chrysin derivatives, some of which are more effective aromatase inhibitors than the benchmark compound, aminoglutethimide. Similarly, the reaction of chrysin with various isonitriles and acetylene dicarboxylates results in a new class of flavone derivatives, tricyclic pyrano-flavones which also inhibit human aromatase. Multicomponent reactions involving flavones therefore enable the synthesis of a variety of derivatives, some of which may be useful as anticancer agents.

Novel triazole-tetrahydroisoquinoline hybrids as human aromatase inhibitors

2019 ◽  
Vol 93 ◽  
pp. 103327 ◽  
Author(s):  
Chanamon Chamduang ◽  
Ratchanok Pingaew ◽  
Veda Prachayasittikul ◽  
Supaluk Prachayasittikul ◽  
Somsak Ruchirawat ◽  
...  
Keyword(s):  
Aromatase Inhibitors ◽  
Human Aromatase

Evidence for new non-steroidal human aromatase inhibitors and comparison with equine aromatase inhibition for an understanding of the mammalian active site

1998 ◽  
Vol 33 (6) ◽  
pp. 451-462 ◽  
Author(s):  
Pierrick Auvray ◽  
Safa Moslemi ◽  
Pascal Sourdaine ◽  
Sébastien Galopin ◽  
Gilles-Eric Séralini ◽  
...  
Keyword(s):  
Aromatase Inhibitors ◽  
Active Site ◽  
Aromatase Inhibition ◽  
Human Aromatase
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