Synthesis of bicoumarin thiophosphate derivatives as steroid sulfatase inhibitors - Publikacja - MOST Wiedzy

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Synthesis of bicoumarin thiophosphate derivatives as steroid sulfatase inhibitors

Abstrakt

Based on the frameworks of 7-hydroxy-2,3-dihydro-1H-cyclopenta[c]chromen-4-one, 3-hydroxy- 7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one and 3-hydroxy-8,9,10,11-tetrahydro-7H-cyclohepta[c] chromen-6-one, a series of bicoumarin thiophosphate analogs have been synthesized and biologically evaluated. Additionally, their binding modes have been modeled using docking techniques. The inhibitory properties of the synthesized compounds were tested against the STS isolated from human placenta. Most of the new STS inhibitors possessed good activities against STS. In particular, we found that the bis- (6-oxo-7,8,9,10-tetrahydro-6H-benzo[c]chromen-3-yl) hydrogenthiophosphate (10b) produced the largest inhibitory effect, with an IC50 value of 860 nM (an IC50 value of 1 mM for the 665-COUMATE used as a reference). The structure-activity relationships of the synthesized bicoumarin thiophosphate derivatives toward the STS enzyme have been discussed previously.

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Informacje szczegółowe

Kategoria:
Publikacja w czasopiśmie
Typ:
artykuł w czasopiśmie wyróżnionym w JCR
Opublikowano w:
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY nr 101, strony 358 - 366,
ISSN: 0223-5234
Język:
angielski
Rok wydania:
2015
Opis bibliograficzny:
Demkowicz S., Kozak W., Daśko M., Masłyk M., Gielniewski B., Rachoń J.: Synthesis of bicoumarin thiophosphate derivatives as steroid sulfatase inhibitors// EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. -Vol. 101, (2015), s.358-366
DOI:
Cyfrowy identyfikator dokumentu elektronicznego (otwiera się w nowej karcie) 10.1016/j.ejmech.2015.06.051
Weryfikacja:
Politechnika Gdańska

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