13196-10-6Relevant articles and documents
Synthetic models related to methoxalen and menthofuran-cytochrome P450 (CYP) 2A6 interactions. Benzofuran and coumarin derivatives as potent and selective inhibitors of CYP2A6
Yamaguchi, Yuki,Akimoto, Ichie,Motegi, Kyoko,Yoshimura, Teruki,Wada, Keiji,Nishizono, Naozumi,Oda, Kazuaki
, p. 997 - 1001 (2013)
Human microsomal cytochrome P450 (CYP) 2A6 contributes extensively to nicotine detoxication but also activates tobacco-specific procarcinogens to mutagenic products. We prepared a series of benzofuran and coumarin derivatives that have inhibitory effects on the activity of human CYP2A6. The reported compounds methoxalen and menthofuran had potent inhibitory effects on the activity of CYP2A6 with IC50 values of 0.47 μM and 1.27 μM, respectively. Synthetic benzofuran (4-methoxybenzofuran: IC50=2.20 μM) and coumarin (5-methoxycoumarin: IC50=0.13 μM and 6-methoxycoumarin: IC50=0.64 μM) derivatives, which have more selective effects than those of methoxalen and menthofuran, exhibited comparable activities against CYP2A6. These compounds can be used as a lead compounds in the design of CYP2A6 inhibitor drugs to reduce smoking and tobacco-related cancers.
Facile entry to 4- and 5-hydroxybenzofuran and to their amino derivatives
Bonini, Carlo,Cristiani, Graziella,Funicello, Maria,Viggiani, Licia
, p. 1983 - 1990 (2006)
An innovative one-step procedure for the synthesis of 4-hydroxybenzofuran and an improved synthesis of 5-hydroxybenzofuran is reported. Such compounds were also transformed into their amino derivatives via Smiles rearrangement with good to high overall yields. Copyright Taylor & Francis Group, LLC.
2-Nitrofurans as dienophiles in Diels-Alder reactions
Rosa, Claudia Della,Kneeteman, María N.,Mancini, Pedro M.E.
, p. 8711 - 8714 (2005)
α-Nitrofuran derivatives are studied in Diels-Alder reactions under thermal conditions. In contrast to α-acylfurans, they proved to be efficient dienophiles.
TRICYCLIC SUBSTITUTED PIPERIDINE DIONE COMPOUND
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Paragraph 0101-0102, (2021/07/17)
Disclosed is a series of tricyclic substituted piperidine dione compounds, and applications thereof in the preparation of medicines for treating diseases related to CRBN protein; specifically disclosed are the derivative compound represented by formula (I) or a pharmaceutically acceptable salt thereof.
Immunoproteasome Inhibitor-Doxorubicin Conjugates Target Multiple Myeloma Cells and Release Doxorubicin upon Low-Dose Photon Irradiation
Dekker, Patrick M.,Florea, Bogdan I.,Maiorana, Santina,Maurits, Elmer,Neefjes, Jacques J. C.,Overkleeft, Herman S.,Van De Graaff, Michel J.,Van Der Zanden, Sabina Y.,Van Kasteren, Sander I.,Wander, Dennis P. A.
, p. 7250 - 7253 (2020/08/06)
Proteasome inhibitors are established therapeutic agents for the treatment of hematological cancers, as are anthracyclines such as doxorubicin. We here present a new drug targeting approach that combines both drug classes into a single molecule. Doxorubicin was conjugated to an immunoproteasome-selective inhibitor via light-cleavable linkers, yielding peptide epoxyketone-doxorubicin prodrugs that remained selective and active toward immunoproteasomes. Upon cellular uptake and immunoproteasome inhibition, doxorubicin is released from the immunoproteasome inhibitor through photoirradiation. Multiple myeloma cells in this way take a double hit: immunoproteasome inhibition and doxorubicin-induced toxicity. Our strategy, which entails targeting of a cytotoxic agent, through a covalent enzyme inhibitor that is detrimental to tumor tissue in its own right, may find use in the search for improved anticancer drugs.
Stable crystalline form A of B-RAF kinase dimer inhibitor
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, (2020/08/18)
The invention relates to a stable crystalline form A of a B-RAF kinase dimer inhibitor 1-((1S, 1aS, 6bS)-5-((7-oxo-5, 6, 7, 8-tetrahydro-1, 8-diazanaphthalene-4-yl) oxy)-1a, 6b-dihydro-1H-cyclopropyl[b] benzofuran-1-yl)-3-(2, 4, 5- trifluorophenyl) urea (hereinafter sometimes referred to as a compound 1), a preparation method of the crystalline Form A and therapeutic use of the crystalline Form A.
