- Probing cytochrome P450 (CYP) bioactivation with chloromethylindoline bioprecursors derived from the duocarmycin family of compounds
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The duocarmycins belong to a class of agent which has great potential for use in cancer therapy. Their exquisite potency means they are too toxic for systemic use, and targeted approaches are required to unlock their clinical potential. In this study, we
- Ortuzar, Natalia,Karu, Kersti,Presa, Daniela,Morais, Goreti R.,Sheldrake, Helen M.,Shnyder, Steve D.,Barnieh, Francis M.,Loadman, Paul M.,Patterson, Laurence H.,Pors, Klaus,Searcey, Mark
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supporting information
(2021/05/04)
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- Indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, pyrazolopyridines, isothiazolopyridines, and preparation and uses thereof
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The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (e.g., indazoles and benzothiazoles), which act as ligands for the α7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
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Page/Page column 68
(2010/11/26)
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- 1 H-INDAZOLES, BENZOTHIAZOLES, 1,2-BENZOISOXAZOLES, 1,2-BENZOISOTHIAZOLES, AND CHROMONES AND PREPARATION AND USES THEREOF
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The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of -disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the α7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
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Page/Page column 78
(2010/11/27)
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- AN ALTERNATIVE METHOD FOR SYNTHESIS OF THE CC-1065 PHARMACOPHORE, 1,2,7,7a-TETRAHYDROCYCLOPROPINDOL-4-ONE
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The synthesis of the CC-1065 pharmacophore, 2-(1-methylpyrrole-2-carbonyl)-1,2,7,7a-tetrahydrocyclopropindol-4-one (17), is described.The methods reported here provide an alternative route for the synthesis of compounds possessing the biologically
- Wang, Yugiang,Lown, J. William
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p. 1399 - 1410
(2007/10/02)
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- Stereoelectronic factors influencing the biological activity and DNA interaction of synthetic antitumor agents modeled on CC-1065
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The synthesis, physicochemical properties, and biological activities of a series of novel spiro cyclopropyl compounds, modeled on the potent antitumor antibiotic CC-1065 (1), are described. Many of these synthetic analogues are significantly more effectiv
- Warpehoski,Gebhard,Kelly,Krueger,Li,McGovren,Prairie,Wicnienski,Wierenga
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p. 590 - 603
(2007/10/02)
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