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Literature summary for 1.1.1.88 extracted from

  • Perchellet, J.P.; Perchellet, E.M.; Crow, K.R.; Buszek, K.R.; Brown, N.; Ellappan, S.; Gao, G.; Luo, D.; Minatoya, M.; Lushington, G.H.
    Novel synthetic inhibitors of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase activity that inhibit tumor cell proliferation and are structurally unrelated to existing statins (2009), Int. J. Mol. Med., 24, 633-643.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
(3S,6Z)-3-benzyl-1-(4-fluorobenzyl)-8-(4-methoxyphenyl)-4-(3-methylbutanoyl)-3,4,5,8-tetrahydro-1,4-diazocin-2(1H)-one purified enzyme, 52.6% residual activity at 0.01 mM Homo sapiens
(3S,6Z)-3-benzyl-1-(4-fluorobenzyl)-8-(4-methoxyphenyl)-4-(3-methylbutanoyl)-3,4,5,8-tetrahydro-1,4-diazocin-2(1H)-one antiproliferative activity in L-1210 cell, IC50 0.00148 mM Mus musculus
(3S,6Z)-3-benzyl-1-(4-fluorobenzyl)-8-(4-methoxyphenyl)-4-[[(E)-2-phenylethenyl]sulfonyl]-3,4,5,8-tetrahydro-1,4-diazocin-2(1H)-one purified enzyme, 32.3% residual activity at 0.01 mM Homo sapiens
(3S,6Z)-3-benzyl-1-(4-fluorobenzyl)-8-(4-methoxyphenyl)-4-[[(E)-2-phenylethenyl]sulfonyl]-3,4,5,8-tetrahydro-1,4-diazocin-2(1H)-one antiproliferative activity in L-1210 cell, IC50 0.0023 mM Mus musculus
(3S,6Z)-3-benzyl-4-(3,3-dimethylbutanoyl)-1-(4-fluorobenzyl)-8-(4-methoxyphenyl)-3,4,5,8-tetrahydro-1,4-diazocin-2(1H)-one purified enzyme, 43.4% residual activity at 0.01 mM Homo sapiens
(3S,6Z)-3-benzyl-4-(3,3-dimethylbutanoyl)-1-(4-fluorobenzyl)-8-(4-methoxyphenyl)-3,4,5,8-tetrahydro-1,4-diazocin-2(1H)-one antiproliferative activity in L-1210 cell, IC50 0.00143 mM Mus musculus
(3S,6Z)-4-(biphenyl-4-ylsulfonyl)-1-(4-fluorobenzyl)-8-(4-methoxyphenyl)-3-methyl-3,4,5,8-tetrahydro-1,4-diazocin-2(1H)-one purified enzyme, 54.4% residual activity at 0.01 mM Homo sapiens
(3S,6Z)-4-(biphenyl-4-ylsulfonyl)-1-(4-fluorobenzyl)-8-(4-methoxyphenyl)-3-methyl-3,4,5,8-tetrahydro-1,4-diazocin-2(1H)-one antiproliferative activity in L-1210 cell, IC50 0.00119 mM Mus musculus

Organism

Organism UniProt Comment Textmining
Homo sapiens
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Mus musculus
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Purification (Commentary)

Purification (Comment) Organism
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Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
L-1210 cell
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Mus musculus
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