- Tetrahydroquinazoline Derivatives Useful as Anticancer Agents
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Compounds of the general formula: processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.
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Paragraph 0211; 0212
(2019/08/26)
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- Modular Total Synthesis and Cell-Based Anticancer Activity Evaluation of Ouabagenin and Other Cardiotonic Steroids with Varying Degrees of Oxygenation
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A Cu(II)-catalyzed diastereoselective Michael/aldol cascade approach is used to accomplish concise total syntheses of cardiotonic steroids with varying degrees of oxygenation including cardenolides ouabagenin, sarmentologenin, 19-hydroxysarmentogenin, and 5-epi-panogenin. These syntheses enabled the subsequent structure activity relationship (SAR) studies on 37 synthetic and natural steroids to elucidate the effect of oxygenation, stereochemistry, C3-glycosylation, and C17-heterocyclic ring. Based on this parallel evaluation of synthetic and natural steroids and their derivatives, glycosylated steroids cannogenol-l-α-rhamnoside (79a), strophanthidol-l-α-rhamnoside (92), and digitoxigenin-l-α-rhamnoside (97) were identified as the most potent steroids demonstrating broad anticancer activity at 10-100 nM concentrations and selectivity (nontoxic at 3 μM against NIH-3T3, MEF, and developing fish embryos). Further analyses indicate that these molecules show a general mode of anticancer activity involving DNA-damage upregulation that subsequently induces apoptosis.
- Khatri, Hem Raj,Bhattarai, Bijay,Kaplan, Will,Li, Zhongzheng,Curtis Long, Marcus John,Aye, Yimon,Nagorny, Pavel
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p. 4849 - 4860
(2019/03/26)
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- Enantioselective Total Synthesis of Cannogenol-3-O-α- l -rhamnoside via Sequential Cu(II)-Catalyzed Michael Addition/Intramolecular Aldol Cyclization Reactions
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A concise and scalable enantioselective total synthesis of the natural cardenolides cannogenol and cannogenol-3-O-α-l-rhamnoside has been achieved in 18 linear steps. The synthesis features a Cu(II)-catalyzed enantioselective and diastereoselective Michae
- Bhattarai, Bijay,Nagorny, Pavel
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supporting information
p. 154 - 157
(2018/01/17)
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- Diastereoselective construction of 7-methylenebicyclo[3.2.1]oct-3-en-2-one derivatives by palladium-catalyzed cyclization of propargylic acetates with 2-oxocyclohex-3-enecarboxylates
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The reaction of propargylic acetates with 2-oxocyclohex-3-enecarboxylates in the presence of a palladium catalyst is described. Substituted 7-methylenebicyclo[3.2.1]oct-3-en-2-ones were synthesized in a highly diastereoselective manner.
- Yoshida, Masahiro,Sugimura, Chiyuki,Shishido, Kozo
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supporting information; experimental part
p. 3482 - 3485
(2011/09/13)
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- Design, synthesis, structure, and dehydrogenation reactivity of a water soluble o-iodoxybenzoic acid derivative bearing a trimethylammonium group
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5-Trimethylammonio-1, 3-dioxo-1, 3-dihydro-1λ5-benzo[d][1, 2]iodoxol-1-ol anion (AIBX 1a), an o-iodoxybenzoic acid (IBX) derivative having the trimethylammonium moiety on its phenyl ring, possesses very good solubility in water and distinct oxidative properties from IBX, which is demonstrated in the oxidation of various β-keto esters to the corresponding dehydrogenated products using water as cosolvent. The regeneration of AIBX 1a can be easily realized from the reaction mixture due to its good water solubility.2011 American Chemical Society.
- Cui, Li-Qian,Dong, Zhi-Lei,Liu, Kai,Zhang, Chi
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supporting information; experimental part
p. 6488 - 6491
(2012/02/02)
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- PYRIMIDINE COMPOUNDS AS SEROTONIN RECEPTOR MODULATORS
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Certain pyrimidine-containing compounds are serotonin receptor modulators useful in the treatment of serotonin-mediated diseases.
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Page/Page column 36
(2008/06/13)
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- N-UREIDOALKYL-AMINO COMPOUNDS AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
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The present application describes modulators of chemokine receptors of formula (I), or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
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Page/Page column 154-155
(2008/06/13)
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- N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
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The present application describes modulators of chemokine receptor activity of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases, as well as autoimmune pathologies such as rheum
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