Tao, Zeyu published the artcileDesign, synthesis and in vitro anti-Zika virus evaluation of novel Sinefungin derivatives, Synthetic Route of 1338466-77-5, the publication is European Journal of Medicinal Chemistry (2018), 994-1004, database is CAplus and MEDLINE.
We report herein the design and synthesis of a series of novel Sinefungin (SIN) derivatives, based on the structures of SIN and its analog EPZ004777. Our results reveal that target compounds(I) (R1 = F, R2 = 4-t-Bu-C6H4, 4-CF3-C6H4, 3-CF3-C6H4; R1 = Cl, R2 = 4-F-C6H4, 4-Me-C6H4, 3-CF3-C6H4, tert-Bu, cyclohexyl) show better activity (IC50 = 4.56-20.16 μM) than EPZ004777 (IC50 = 35.19 μM). Surprisingly, SIN was founded to be not as active (IC50 > 50 μM) as we and other research groups predicted. Interestingly, the intermediates (II) and (III) (R1 = F, Cl) display potent anti-ZIKV potency (IC50 = 6.33-29.98 μM), and compound II (R1 = F) also exhibits acceptable cytotoxicity (CC50 > 200 μM), suggesting their promising potential to be leads for further development.
European Journal of Medicinal Chemistry published new progress about 1338466-77-5. 1338466-77-5 belongs to tetrahydrofurans, auxiliary class Epigenetics,Histone Methyltransferase, name is 1-(3-((((2R,3S,4R,5R)-5-(4-Amino-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl)(isopropyl)amino)propyl)-3-(4-(tert-butyl)phenyl)urea, and the molecular formula is C28H29NO4, Synthetic Route of 1338466-77-5.
Referemce:
https://en.wikipedia.org/wiki/Tetrahydrofuran,
Tetrahydrofuran | (CH2)3CH2O – PubChem