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Tumor-selective cytotoxicity of a novel pentadiene analogue on human leukemia/ lymphoma cells.
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BACKGROUND
A novel series of structurally divergent 1,5-diaryl-3-oxo-1,4-pentadiene analogues 1-10 displayed marked cytotoxic potencies towards a number of human leukemia/lymphoma cells.
OBJECTIVE
To identify novel selective cytotoxic compounds that induce apoptosis.
METHODS
The Differential Nuclear
Isolation, structure elucidation and total synthesis of a cytotoxic dienone from Echinacea pallida.
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The isolation and structure characterization of a dienone from the roots of Echinacea pallida, namely (8Z,11Z)-pentadeca-8,11-dien-2-one, are described here. To assess the configuration of this secondary metabolite, the stereoselective total synthesis of the two isomeric forms, (8Z,11Z)- and
Antiproliferative and cytotoxic effects of newly discovered halogenated coral prostanoids from the Japanese stolonifer Clavularia viridis on human myeloid leukemia cells in culture.
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The antiproliferative and cytotoxic activities of newly discovered halogenated coral prostanoids (chlorovulone, bromovulone, and iodovulone) from the Japanese stolonifer Clavularia viridis and their related compounds were determined in HL-60 cells in culture. The order of antiproliferative and
Cyclopentenone prostaglandins with dienone structure promote cross-linking of the chemoresistance-inducing enzyme glutathione transferase P1-1.
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Glutathione transferase P1-1 (GSTP1-1) plays crucial roles in cancer chemoprevention and chemoresistance and is a key target for anticancer drug development. Oxidative stress or inhibitor-induced GSTP1-1 oligomerization leads to the activation of stress cascades and apoptosis in various tumor cells.
Structure requirements for antiproliferative and cytotoxic activities of marine coral prostanoids from the Japanese stolonifer Clavularia viridis against human myeloid leukemia cells in culture.
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The structural requirements for antiproliferative and cytotoxic activities of marine coral prostanoids from Japanese stolonifer Clavularia viridis and related compounds were examined in HL-60 cells in culture. From our data on the structure-activity relationship of these compounds, we elucidated
Novel 3,5-bis(arylidene)-4-oxo-1-piperidinyl dimers: structure-activity relationships and potent antileukemic and antilymphoma cytotoxicity.
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Novel clusters of 3,5-bis(benzylidene)-4-oxo-1-piperidinyl dimers 3-5 were evaluated against human Molt4/C8 and CEM T-lymphocytes and human HeLa cervix adenocarcinoma cells as well as murine L1210 leukemia neoplasms. Several of these compounds demonstrated IC50 values in the submicromolar and low
Total Synthesis of Δ(12) -Prostaglandin J3 : Evolution of Synthetic Strategies to a Streamlined Process.
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The total synthesis of Δ(12) -prostaglandin J3 (Δ(12) -PGJ3 , 1), a reported leukemia stem cell ablator, through a number of strategies and tactics is described. The signature cross-conjugated dienone structural motif of 1 was forged by an aldol reaction/dehydration sequence from key building blocks
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