The Experts below are selected from a list of 603 Experts worldwide ranked by ideXlab platform
Tadashi Honda - One of the best experts on this subject based on the ideXlab platform.
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New Monocyclic, Bicyclic, and Tricyclic Ethynylcyanodienones as Activators of the Keap1/Nrf2/ARE Pathway and Inhibitors of Inducible Nitric Oxide Synthase.
Journal of medicinal chemistry, 2015Co-Authors: Suqing Zheng, Maureen Higgins, Rocco P. Morra, Anne T. Mendis, Chih-wei Chien, Iwao Ojima, Dale F. Mierke, Albena T. Dinkova-kostova, Tadashi HondaAbstract:A Monocyclic Compound 3 (3-ethynyl-3-methyl-6-oxocyclohexa-1,4-dienecarbonitrile) is a highly reactive Michael acceptor leading to reversible adducts with nucleophiles, which displays equal or greater potency than the pentacyclic triterpenoid CDDO in inflammation and carcinogenesis related assays. Recently, reversible covalent drugs, which bind with protein targets but not permanently, have been gaining attention because of their unique features. To explore such reversible covalent drugs, we have synthesized Monocyclic, bicyclic, and tricyclic Compounds containing 3 as an electrophilic fragment and evaluated them as activators of the Keap1/Nrf2/ARE pathway and inhibitors of iNOS. Notably, these Compounds maintain the unique features of the chemical reactivity and biological potency of 3. Among them, a Monocyclic Compound 5 is the most potent in these assays while a tricyclic Compound 14 displays a more robust and specific activation profile compared to 5. In conclusion, we demonstrate that 3 is a useful e...
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New Monocyclic, Bicyclic, and Tricyclic Ethynylcyanodienones as Activators of the Keap1/Nrf2/ARE Pathway and Inhibitors of Inducible Nitric Oxide Synthase
2015Co-Authors: Suqing Zheng, Maureen Higgins, Rocco P. Morra, Anne T. Mendis, Chih-wei Chien, Iwao Ojima, Dale F. Mierke, Albena T. Dinkova-kostova, Tadashi HondaAbstract:A Monocyclic Compound 3 (3-ethynyl-3-methyl-6-oxocyclohexa-1,4-dienecarbonitrile) is a highly reactive Michael acceptor leading to reversible adducts with nucleophiles, which displays equal or greater potency than the pentacyclic triterpenoid CDDO in inflammation and carcinogenesis related assays. Recently, reversible covalent drugs, which bind with protein targets but not permanently, have been gaining attention because of their unique features. To explore such reversible covalent drugs, we have synthesized Monocyclic, bicyclic, and tricyclic Compounds containing 3 as an electrophilic fragment and evaluated them as activators of the Keap1/Nrf2/ARE pathway and inhibitors of iNOS. Notably, these Compounds maintain the unique features of the chemical reactivity and biological potency of 3. Among them, a Monocyclic Compound 5 is the most potent in these assays while a tricyclic Compound 14 displays a more robust and specific activation profile compared to 5. In conclusion, we demonstrate that 3 is a useful electrophilic fragment for exploring reversible covalent drugs
Suqing Zheng - One of the best experts on this subject based on the ideXlab platform.
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New Monocyclic, Bicyclic, and Tricyclic Ethynylcyanodienones as Activators of the Keap1/Nrf2/ARE Pathway and Inhibitors of Inducible Nitric Oxide Synthase.
Journal of medicinal chemistry, 2015Co-Authors: Suqing Zheng, Maureen Higgins, Rocco P. Morra, Anne T. Mendis, Chih-wei Chien, Iwao Ojima, Dale F. Mierke, Albena T. Dinkova-kostova, Tadashi HondaAbstract:A Monocyclic Compound 3 (3-ethynyl-3-methyl-6-oxocyclohexa-1,4-dienecarbonitrile) is a highly reactive Michael acceptor leading to reversible adducts with nucleophiles, which displays equal or greater potency than the pentacyclic triterpenoid CDDO in inflammation and carcinogenesis related assays. Recently, reversible covalent drugs, which bind with protein targets but not permanently, have been gaining attention because of their unique features. To explore such reversible covalent drugs, we have synthesized Monocyclic, bicyclic, and tricyclic Compounds containing 3 as an electrophilic fragment and evaluated them as activators of the Keap1/Nrf2/ARE pathway and inhibitors of iNOS. Notably, these Compounds maintain the unique features of the chemical reactivity and biological potency of 3. Among them, a Monocyclic Compound 5 is the most potent in these assays while a tricyclic Compound 14 displays a more robust and specific activation profile compared to 5. In conclusion, we demonstrate that 3 is a useful e...
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New Monocyclic, Bicyclic, and Tricyclic Ethynylcyanodienones as Activators of the Keap1/Nrf2/ARE Pathway and Inhibitors of Inducible Nitric Oxide Synthase
2015Co-Authors: Suqing Zheng, Maureen Higgins, Rocco P. Morra, Anne T. Mendis, Chih-wei Chien, Iwao Ojima, Dale F. Mierke, Albena T. Dinkova-kostova, Tadashi HondaAbstract:A Monocyclic Compound 3 (3-ethynyl-3-methyl-6-oxocyclohexa-1,4-dienecarbonitrile) is a highly reactive Michael acceptor leading to reversible adducts with nucleophiles, which displays equal or greater potency than the pentacyclic triterpenoid CDDO in inflammation and carcinogenesis related assays. Recently, reversible covalent drugs, which bind with protein targets but not permanently, have been gaining attention because of their unique features. To explore such reversible covalent drugs, we have synthesized Monocyclic, bicyclic, and tricyclic Compounds containing 3 as an electrophilic fragment and evaluated them as activators of the Keap1/Nrf2/ARE pathway and inhibitors of iNOS. Notably, these Compounds maintain the unique features of the chemical reactivity and biological potency of 3. Among them, a Monocyclic Compound 5 is the most potent in these assays while a tricyclic Compound 14 displays a more robust and specific activation profile compared to 5. In conclusion, we demonstrate that 3 is a useful electrophilic fragment for exploring reversible covalent drugs
Dale F. Mierke - One of the best experts on this subject based on the ideXlab platform.
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New Monocyclic, Bicyclic, and Tricyclic Ethynylcyanodienones as Activators of the Keap1/Nrf2/ARE Pathway and Inhibitors of Inducible Nitric Oxide Synthase.
Journal of medicinal chemistry, 2015Co-Authors: Suqing Zheng, Maureen Higgins, Rocco P. Morra, Anne T. Mendis, Chih-wei Chien, Iwao Ojima, Dale F. Mierke, Albena T. Dinkova-kostova, Tadashi HondaAbstract:A Monocyclic Compound 3 (3-ethynyl-3-methyl-6-oxocyclohexa-1,4-dienecarbonitrile) is a highly reactive Michael acceptor leading to reversible adducts with nucleophiles, which displays equal or greater potency than the pentacyclic triterpenoid CDDO in inflammation and carcinogenesis related assays. Recently, reversible covalent drugs, which bind with protein targets but not permanently, have been gaining attention because of their unique features. To explore such reversible covalent drugs, we have synthesized Monocyclic, bicyclic, and tricyclic Compounds containing 3 as an electrophilic fragment and evaluated them as activators of the Keap1/Nrf2/ARE pathway and inhibitors of iNOS. Notably, these Compounds maintain the unique features of the chemical reactivity and biological potency of 3. Among them, a Monocyclic Compound 5 is the most potent in these assays while a tricyclic Compound 14 displays a more robust and specific activation profile compared to 5. In conclusion, we demonstrate that 3 is a useful e...
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New Monocyclic, Bicyclic, and Tricyclic Ethynylcyanodienones as Activators of the Keap1/Nrf2/ARE Pathway and Inhibitors of Inducible Nitric Oxide Synthase
2015Co-Authors: Suqing Zheng, Maureen Higgins, Rocco P. Morra, Anne T. Mendis, Chih-wei Chien, Iwao Ojima, Dale F. Mierke, Albena T. Dinkova-kostova, Tadashi HondaAbstract:A Monocyclic Compound 3 (3-ethynyl-3-methyl-6-oxocyclohexa-1,4-dienecarbonitrile) is a highly reactive Michael acceptor leading to reversible adducts with nucleophiles, which displays equal or greater potency than the pentacyclic triterpenoid CDDO in inflammation and carcinogenesis related assays. Recently, reversible covalent drugs, which bind with protein targets but not permanently, have been gaining attention because of their unique features. To explore such reversible covalent drugs, we have synthesized Monocyclic, bicyclic, and tricyclic Compounds containing 3 as an electrophilic fragment and evaluated them as activators of the Keap1/Nrf2/ARE pathway and inhibitors of iNOS. Notably, these Compounds maintain the unique features of the chemical reactivity and biological potency of 3. Among them, a Monocyclic Compound 5 is the most potent in these assays while a tricyclic Compound 14 displays a more robust and specific activation profile compared to 5. In conclusion, we demonstrate that 3 is a useful electrophilic fragment for exploring reversible covalent drugs
Albena T. Dinkova-kostova - One of the best experts on this subject based on the ideXlab platform.
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New Monocyclic, Bicyclic, and Tricyclic Ethynylcyanodienones as Activators of the Keap1/Nrf2/ARE Pathway and Inhibitors of Inducible Nitric Oxide Synthase.
Journal of medicinal chemistry, 2015Co-Authors: Suqing Zheng, Maureen Higgins, Rocco P. Morra, Anne T. Mendis, Chih-wei Chien, Iwao Ojima, Dale F. Mierke, Albena T. Dinkova-kostova, Tadashi HondaAbstract:A Monocyclic Compound 3 (3-ethynyl-3-methyl-6-oxocyclohexa-1,4-dienecarbonitrile) is a highly reactive Michael acceptor leading to reversible adducts with nucleophiles, which displays equal or greater potency than the pentacyclic triterpenoid CDDO in inflammation and carcinogenesis related assays. Recently, reversible covalent drugs, which bind with protein targets but not permanently, have been gaining attention because of their unique features. To explore such reversible covalent drugs, we have synthesized Monocyclic, bicyclic, and tricyclic Compounds containing 3 as an electrophilic fragment and evaluated them as activators of the Keap1/Nrf2/ARE pathway and inhibitors of iNOS. Notably, these Compounds maintain the unique features of the chemical reactivity and biological potency of 3. Among them, a Monocyclic Compound 5 is the most potent in these assays while a tricyclic Compound 14 displays a more robust and specific activation profile compared to 5. In conclusion, we demonstrate that 3 is a useful e...
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New Monocyclic, Bicyclic, and Tricyclic Ethynylcyanodienones as Activators of the Keap1/Nrf2/ARE Pathway and Inhibitors of Inducible Nitric Oxide Synthase
2015Co-Authors: Suqing Zheng, Maureen Higgins, Rocco P. Morra, Anne T. Mendis, Chih-wei Chien, Iwao Ojima, Dale F. Mierke, Albena T. Dinkova-kostova, Tadashi HondaAbstract:A Monocyclic Compound 3 (3-ethynyl-3-methyl-6-oxocyclohexa-1,4-dienecarbonitrile) is a highly reactive Michael acceptor leading to reversible adducts with nucleophiles, which displays equal or greater potency than the pentacyclic triterpenoid CDDO in inflammation and carcinogenesis related assays. Recently, reversible covalent drugs, which bind with protein targets but not permanently, have been gaining attention because of their unique features. To explore such reversible covalent drugs, we have synthesized Monocyclic, bicyclic, and tricyclic Compounds containing 3 as an electrophilic fragment and evaluated them as activators of the Keap1/Nrf2/ARE pathway and inhibitors of iNOS. Notably, these Compounds maintain the unique features of the chemical reactivity and biological potency of 3. Among them, a Monocyclic Compound 5 is the most potent in these assays while a tricyclic Compound 14 displays a more robust and specific activation profile compared to 5. In conclusion, we demonstrate that 3 is a useful electrophilic fragment for exploring reversible covalent drugs
Maureen Higgins - One of the best experts on this subject based on the ideXlab platform.
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New Monocyclic, Bicyclic, and Tricyclic Ethynylcyanodienones as Activators of the Keap1/Nrf2/ARE Pathway and Inhibitors of Inducible Nitric Oxide Synthase.
Journal of medicinal chemistry, 2015Co-Authors: Suqing Zheng, Maureen Higgins, Rocco P. Morra, Anne T. Mendis, Chih-wei Chien, Iwao Ojima, Dale F. Mierke, Albena T. Dinkova-kostova, Tadashi HondaAbstract:A Monocyclic Compound 3 (3-ethynyl-3-methyl-6-oxocyclohexa-1,4-dienecarbonitrile) is a highly reactive Michael acceptor leading to reversible adducts with nucleophiles, which displays equal or greater potency than the pentacyclic triterpenoid CDDO in inflammation and carcinogenesis related assays. Recently, reversible covalent drugs, which bind with protein targets but not permanently, have been gaining attention because of their unique features. To explore such reversible covalent drugs, we have synthesized Monocyclic, bicyclic, and tricyclic Compounds containing 3 as an electrophilic fragment and evaluated them as activators of the Keap1/Nrf2/ARE pathway and inhibitors of iNOS. Notably, these Compounds maintain the unique features of the chemical reactivity and biological potency of 3. Among them, a Monocyclic Compound 5 is the most potent in these assays while a tricyclic Compound 14 displays a more robust and specific activation profile compared to 5. In conclusion, we demonstrate that 3 is a useful e...
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New Monocyclic, Bicyclic, and Tricyclic Ethynylcyanodienones as Activators of the Keap1/Nrf2/ARE Pathway and Inhibitors of Inducible Nitric Oxide Synthase
2015Co-Authors: Suqing Zheng, Maureen Higgins, Rocco P. Morra, Anne T. Mendis, Chih-wei Chien, Iwao Ojima, Dale F. Mierke, Albena T. Dinkova-kostova, Tadashi HondaAbstract:A Monocyclic Compound 3 (3-ethynyl-3-methyl-6-oxocyclohexa-1,4-dienecarbonitrile) is a highly reactive Michael acceptor leading to reversible adducts with nucleophiles, which displays equal or greater potency than the pentacyclic triterpenoid CDDO in inflammation and carcinogenesis related assays. Recently, reversible covalent drugs, which bind with protein targets but not permanently, have been gaining attention because of their unique features. To explore such reversible covalent drugs, we have synthesized Monocyclic, bicyclic, and tricyclic Compounds containing 3 as an electrophilic fragment and evaluated them as activators of the Keap1/Nrf2/ARE pathway and inhibitors of iNOS. Notably, these Compounds maintain the unique features of the chemical reactivity and biological potency of 3. Among them, a Monocyclic Compound 5 is the most potent in these assays while a tricyclic Compound 14 displays a more robust and specific activation profile compared to 5. In conclusion, we demonstrate that 3 is a useful electrophilic fragment for exploring reversible covalent drugs