The Experts below are selected from a list of 11517 Experts worldwide ranked by ideXlab platform
John Drewe - One of the best experts on this subject based on the ideXlab platform.
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discovery characterization and sar of gambogic acid as a potent apoptosis inducer by a hts assay
Bioorganic & Medicinal Chemistry, 2004Co-Authors: Hanzhong Zhang, John Guastella, John Herich, Ben Tseng, Shailaja Kasibhatla, Yan Wang, John DreweAbstract:Gambogic acid (2), a natural product isolated from the resin of Garcinia hurburyi tree, was discovered to be a potent apoptosis inducer using our cell- and caspase-based high-throughput screening assays. Gambogic acid was found to have an EC50 of 0.78 μM in the caspase activation assay in T47D breast cancer cells. The apoptosis-inducing activity of gambogic acid was further characterized by a nuclear fragmentation assay and flow cytometry analysis in human breast tumor cells T47D. Gambogic acid was found to induce apoptosis independent of cell cycle, which is different from paclitaxel that arrests cells in the G2/M phase. To understand the structure–activity relationship (SAR) of gambogic acid, derivatives of 2 with modifications to different function groups were prepared. SAR studies of gambogic acid, as measured by the caspase activation assay, showed that the 9,10 Carbon–Carbon Double Bond of the α,β-unsaturated ketone is important for biological activity, while the 6-hydroxy and 30-carboxy group can tolerate a variety of modifications. The importance of the 9,10 Carbon–Carbon Double Bond was confirmed by the traditional growth inhibition assay. The high potency of 2 as an inducer of apoptosis, its novel mechanism of action, easy isolation and abundant supply, as well as the fact that it is amenable to chemical modification, makes gambogic acid an attractive molecule for the development of anticancer agents.
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discovery characterization and sar of gambogic acid as a potent apoptosis inducer by a hts assay
Bioorganic & Medicinal Chemistry, 2004Co-Authors: Hanzhong Zhang, John Guastella, John Herich, Ben Tseng, Shailaja Kasibhatla, Yan Wang, John DreweAbstract:Gambogic acid (2), a natural product isolated from the resin of Garcinia hurburyi tree, was discovered to be a potent apoptosis inducer using our cell- and caspase-based high-throughput screening assays. Gambogic acid was found to have an EC50 of 0.78 μM in the caspase activation assay in T47D breast cancer cells. The apoptosis-inducing activity of gambogic acid was further characterized by a nuclear fragmentation assay and flow cytometry analysis in human breast tumor cells T47D. Gambogic acid was found to induce apoptosis independent of cell cycle, which is different from paclitaxel that arrests cells in the G2/M phase. To understand the structure–activity relationship (SAR) of gambogic acid, derivatives of 2 with modifications to different function groups were prepared. SAR studies of gambogic acid, as measured by the caspase activation assay, showed that the 9,10 Carbon–Carbon Double Bond of the α,β-unsaturated ketone is important for biological activity, while the 6-hydroxy and 30-carboxy group can tolerate a variety of modifications. The importance of the 9,10 Carbon–Carbon Double Bond was confirmed by the traditional growth inhibition assay. The high potency of 2 as an inducer of apoptosis, its novel mechanism of action, easy isolation and abundant supply, as well as the fact that it is amenable to chemical modification, makes gambogic acid an attractive molecule for the development of anticancer agents.
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discovery characterization and sar of gambogic acid as a potent apoptosis inducer by a hts assay
Bioorganic & Medicinal Chemistry, 2004Co-Authors: Hanzhong Zhang, John Guastella, John Herich, John Drewe, Ben Tseng, Shailaja Kasibhatla, Yan Wang, Sui Xiong CaiAbstract:Gambogic acid (2), a natural product isolated from the resin of Garcinia hurburyi tree, was discovered to be a potent apoptosis inducer using our cell- and caspase-based high-throughput screening assays. Gambogic acid was found to have an EC(50) of 0.78 microM in the caspase activation assay in T47D breast cancer cells. The apoptosis-inducing activity of gambogic acid was further characterized by a nuclear fragmentation assay and flow cytometry analysis in human breast tumor cells T47D. Gambogic acid was found to induce apoptosis independent of cell cycle, which is different from paclitaxel that arrests cells in the G2/M phase. To understand the structure-activity relationship (SAR) of gambogic acid, derivatives of 2 with modifications to different function groups were prepared. SAR studies of gambogic acid, as measured by the caspase activation assay, showed that the 9,10 Carbon-Carbon Double Bond of the alpha,beta-unsaturated ketone is important for biological activity, while the 6-hydroxy and 30-carboxy group can tolerate a variety of modifications. The importance of the 9,10 Carbon-Carbon Double Bond was confirmed by the traditional growth inhibition assay. The high potency of 2 as an inducer of apoptosis, its novel mechanism of action, easy isolation and abundant supply, as well as the fact that it is amenable to chemical modification, makes gambogic acid an attractive molecule for the development of anticancer agents.
Hanzhong Zhang - One of the best experts on this subject based on the ideXlab platform.
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discovery characterization and sar of gambogic acid as a potent apoptosis inducer by a hts assay
Bioorganic & Medicinal Chemistry, 2004Co-Authors: Hanzhong Zhang, John Guastella, John Herich, Ben Tseng, Shailaja Kasibhatla, Yan Wang, John DreweAbstract:Gambogic acid (2), a natural product isolated from the resin of Garcinia hurburyi tree, was discovered to be a potent apoptosis inducer using our cell- and caspase-based high-throughput screening assays. Gambogic acid was found to have an EC50 of 0.78 μM in the caspase activation assay in T47D breast cancer cells. The apoptosis-inducing activity of gambogic acid was further characterized by a nuclear fragmentation assay and flow cytometry analysis in human breast tumor cells T47D. Gambogic acid was found to induce apoptosis independent of cell cycle, which is different from paclitaxel that arrests cells in the G2/M phase. To understand the structure–activity relationship (SAR) of gambogic acid, derivatives of 2 with modifications to different function groups were prepared. SAR studies of gambogic acid, as measured by the caspase activation assay, showed that the 9,10 Carbon–Carbon Double Bond of the α,β-unsaturated ketone is important for biological activity, while the 6-hydroxy and 30-carboxy group can tolerate a variety of modifications. The importance of the 9,10 Carbon–Carbon Double Bond was confirmed by the traditional growth inhibition assay. The high potency of 2 as an inducer of apoptosis, its novel mechanism of action, easy isolation and abundant supply, as well as the fact that it is amenable to chemical modification, makes gambogic acid an attractive molecule for the development of anticancer agents.
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discovery characterization and sar of gambogic acid as a potent apoptosis inducer by a hts assay
Bioorganic & Medicinal Chemistry, 2004Co-Authors: Hanzhong Zhang, John Guastella, John Herich, Ben Tseng, Shailaja Kasibhatla, Yan Wang, John DreweAbstract:Gambogic acid (2), a natural product isolated from the resin of Garcinia hurburyi tree, was discovered to be a potent apoptosis inducer using our cell- and caspase-based high-throughput screening assays. Gambogic acid was found to have an EC50 of 0.78 μM in the caspase activation assay in T47D breast cancer cells. The apoptosis-inducing activity of gambogic acid was further characterized by a nuclear fragmentation assay and flow cytometry analysis in human breast tumor cells T47D. Gambogic acid was found to induce apoptosis independent of cell cycle, which is different from paclitaxel that arrests cells in the G2/M phase. To understand the structure–activity relationship (SAR) of gambogic acid, derivatives of 2 with modifications to different function groups were prepared. SAR studies of gambogic acid, as measured by the caspase activation assay, showed that the 9,10 Carbon–Carbon Double Bond of the α,β-unsaturated ketone is important for biological activity, while the 6-hydroxy and 30-carboxy group can tolerate a variety of modifications. The importance of the 9,10 Carbon–Carbon Double Bond was confirmed by the traditional growth inhibition assay. The high potency of 2 as an inducer of apoptosis, its novel mechanism of action, easy isolation and abundant supply, as well as the fact that it is amenable to chemical modification, makes gambogic acid an attractive molecule for the development of anticancer agents.
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discovery characterization and sar of gambogic acid as a potent apoptosis inducer by a hts assay
Bioorganic & Medicinal Chemistry, 2004Co-Authors: Hanzhong Zhang, John Guastella, John Herich, John Drewe, Ben Tseng, Shailaja Kasibhatla, Yan Wang, Sui Xiong CaiAbstract:Gambogic acid (2), a natural product isolated from the resin of Garcinia hurburyi tree, was discovered to be a potent apoptosis inducer using our cell- and caspase-based high-throughput screening assays. Gambogic acid was found to have an EC(50) of 0.78 microM in the caspase activation assay in T47D breast cancer cells. The apoptosis-inducing activity of gambogic acid was further characterized by a nuclear fragmentation assay and flow cytometry analysis in human breast tumor cells T47D. Gambogic acid was found to induce apoptosis independent of cell cycle, which is different from paclitaxel that arrests cells in the G2/M phase. To understand the structure-activity relationship (SAR) of gambogic acid, derivatives of 2 with modifications to different function groups were prepared. SAR studies of gambogic acid, as measured by the caspase activation assay, showed that the 9,10 Carbon-Carbon Double Bond of the alpha,beta-unsaturated ketone is important for biological activity, while the 6-hydroxy and 30-carboxy group can tolerate a variety of modifications. The importance of the 9,10 Carbon-Carbon Double Bond was confirmed by the traditional growth inhibition assay. The high potency of 2 as an inducer of apoptosis, its novel mechanism of action, easy isolation and abundant supply, as well as the fact that it is amenable to chemical modification, makes gambogic acid an attractive molecule for the development of anticancer agents.
Alexey A Popov - One of the best experts on this subject based on the ideXlab platform.
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endohedral fullerene with μ3 carbido ligand and titanium Carbon Double Bond stabilized inside a Carbon cage
Nature Communications, 2014Co-Authors: Anna Svitova, Kamran B Ghiassi, Christin Schlesier, Katrin Junghans, Yang Zhang, Marilyn M Olmstead, Alan L Balch, Lothar Dunsch, Alexey A PopovAbstract:Metallofullerenes typically have polar single Bonds between metals and non-metals. Here, through arc-discharge experiments, the authors observe the formation of an endohedral fullerene with an encapsulated tri-coordinate μ3-Carbon centre and a stable titanium-Carbon Double Bond.
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endohedral fullerene with μ 3 carbido ligand and titanium Carbon Double Bond stabilized inside a Carbon cage
Nature Communications, 2014Co-Authors: Anna Svitova, Kamran B Ghiassi, Christin Schlesier, Katrin Junghans, Yang Zhang, Marilyn M Olmstead, Alan L Balch, Lothar Dunsch, Alexey A PopovAbstract:Metallofullerenes typically have polar single Bonds between metals and non-metals. Here, through arc-discharge experiments, the authors observe the formation of an endohedral fullerene with an encapsulated tri-coordinate μ3-Carbon centre and a stable titanium-Carbon Double Bond.
Narshinha P Argade - One of the best experts on this subject based on the ideXlab platform.
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Diastereoselective Synthesis of (±)-epi-Subincanadine C
2018Co-Authors: Manojkumar G. Kalshetti, Narshinha P ArgadeAbstract:Starting from indolylmaleimide, concise and efficient total synthesis of (±)-epi-subincanadine C was described via stereoselective Wittig olefination, base-induced selective mono-prenylation, regioselective Grignard reaction, diastereoselective Pictet–Spengler cyclization, regioselective oxidative Carbon–Carbon Double-Bond cleavage, one-pot reductions, and intramolecular cyclization pathway. An attempted synthesis of (±)-subincanadine C via diastereoselective Grignard addition to the α,β-unsaturated γ-lactam or diastereoselective reduction of a Carbon–Carbon Double Bond also resulted in yet another route to (±)-epi-subincanadine C
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reactivity umpolung in intramolecular ring closure of 3 4 disubstituted butenolides diastereoselective total synthesis of paeonilide
Organic Letters, 2013Co-Authors: Prashant S Deore, Narshinha P ArgadeAbstract:Remarkable reactivity reversal stratagem in 3,4-disubstituted butenolides under acidic conditions is described. Design of a suitably substituted multifunctional butenolide followed by an acid-catalyzed chemo- and diastereoselective intramolecular ring closure via the reactivity umpolung has been demonstrated to accomplish a concise total synthesis of paeonilide. Overall, the present protocol involves one-pot reduction of an α,β-unsaturated Carbon–Carbon Double Bond and intramolecular nucleophilic insertion of oxygen function at the electron-rich γ-position of butenolide. The involved mechanistic aspects have also been discussed.
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regio and stereoselective selenium dioxide allylic oxidation of e dialkyl alkylidenesuccinates to z allylic alcohols synthesis of natural and unnatural butenolides
ChemInform, 2012Co-Authors: Ramesh M Patel, Vedavati G Puranik, Narshinha P ArgadeAbstract:The butenolides are formed via an exceptional (E)- to (Z)-Carbon—Carbon Double Bond isomerization of the starting succinates.
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regio and stereoselective selenium dioxide allylic oxidation of e dialkyl alkylidenesuccinates to z allylic alcohols synthesis of natural and unnatural butenolides
Organic and Biomolecular Chemistry, 2011Co-Authors: Ramesh M Patel, Vedavati G Puranik, Narshinha P ArgadeAbstract:The first SeO2 induced (Z)-selective allylic alcohol formation of dialkyl alkylidenesuccinates has been demonstrated to accomplish one-step syntheses of several essential butenolides and fused butenolidesvia an unusual E- to Z- Carbon–Carbon Double Bond isomerisation followed by the lactonization pathway. The observed regio- and stereoselective SeO2 allylic oxidation protocol has also been extended to the diastereoselective total synthesis of bioactive natural product isomintlactone, its direct conversion to mintlactone and an example of the base-catalyzed intramolecular rearrangement of γ-lactone to δ-lactone.
Shailaja Kasibhatla - One of the best experts on this subject based on the ideXlab platform.
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discovery characterization and sar of gambogic acid as a potent apoptosis inducer by a hts assay
Bioorganic & Medicinal Chemistry, 2004Co-Authors: Hanzhong Zhang, John Guastella, John Herich, Ben Tseng, Shailaja Kasibhatla, Yan Wang, John DreweAbstract:Gambogic acid (2), a natural product isolated from the resin of Garcinia hurburyi tree, was discovered to be a potent apoptosis inducer using our cell- and caspase-based high-throughput screening assays. Gambogic acid was found to have an EC50 of 0.78 μM in the caspase activation assay in T47D breast cancer cells. The apoptosis-inducing activity of gambogic acid was further characterized by a nuclear fragmentation assay and flow cytometry analysis in human breast tumor cells T47D. Gambogic acid was found to induce apoptosis independent of cell cycle, which is different from paclitaxel that arrests cells in the G2/M phase. To understand the structure–activity relationship (SAR) of gambogic acid, derivatives of 2 with modifications to different function groups were prepared. SAR studies of gambogic acid, as measured by the caspase activation assay, showed that the 9,10 Carbon–Carbon Double Bond of the α,β-unsaturated ketone is important for biological activity, while the 6-hydroxy and 30-carboxy group can tolerate a variety of modifications. The importance of the 9,10 Carbon–Carbon Double Bond was confirmed by the traditional growth inhibition assay. The high potency of 2 as an inducer of apoptosis, its novel mechanism of action, easy isolation and abundant supply, as well as the fact that it is amenable to chemical modification, makes gambogic acid an attractive molecule for the development of anticancer agents.
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discovery characterization and sar of gambogic acid as a potent apoptosis inducer by a hts assay
Bioorganic & Medicinal Chemistry, 2004Co-Authors: Hanzhong Zhang, John Guastella, John Herich, Ben Tseng, Shailaja Kasibhatla, Yan Wang, John DreweAbstract:Gambogic acid (2), a natural product isolated from the resin of Garcinia hurburyi tree, was discovered to be a potent apoptosis inducer using our cell- and caspase-based high-throughput screening assays. Gambogic acid was found to have an EC50 of 0.78 μM in the caspase activation assay in T47D breast cancer cells. The apoptosis-inducing activity of gambogic acid was further characterized by a nuclear fragmentation assay and flow cytometry analysis in human breast tumor cells T47D. Gambogic acid was found to induce apoptosis independent of cell cycle, which is different from paclitaxel that arrests cells in the G2/M phase. To understand the structure–activity relationship (SAR) of gambogic acid, derivatives of 2 with modifications to different function groups were prepared. SAR studies of gambogic acid, as measured by the caspase activation assay, showed that the 9,10 Carbon–Carbon Double Bond of the α,β-unsaturated ketone is important for biological activity, while the 6-hydroxy and 30-carboxy group can tolerate a variety of modifications. The importance of the 9,10 Carbon–Carbon Double Bond was confirmed by the traditional growth inhibition assay. The high potency of 2 as an inducer of apoptosis, its novel mechanism of action, easy isolation and abundant supply, as well as the fact that it is amenable to chemical modification, makes gambogic acid an attractive molecule for the development of anticancer agents.
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discovery characterization and sar of gambogic acid as a potent apoptosis inducer by a hts assay
Bioorganic & Medicinal Chemistry, 2004Co-Authors: Hanzhong Zhang, John Guastella, John Herich, John Drewe, Ben Tseng, Shailaja Kasibhatla, Yan Wang, Sui Xiong CaiAbstract:Gambogic acid (2), a natural product isolated from the resin of Garcinia hurburyi tree, was discovered to be a potent apoptosis inducer using our cell- and caspase-based high-throughput screening assays. Gambogic acid was found to have an EC(50) of 0.78 microM in the caspase activation assay in T47D breast cancer cells. The apoptosis-inducing activity of gambogic acid was further characterized by a nuclear fragmentation assay and flow cytometry analysis in human breast tumor cells T47D. Gambogic acid was found to induce apoptosis independent of cell cycle, which is different from paclitaxel that arrests cells in the G2/M phase. To understand the structure-activity relationship (SAR) of gambogic acid, derivatives of 2 with modifications to different function groups were prepared. SAR studies of gambogic acid, as measured by the caspase activation assay, showed that the 9,10 Carbon-Carbon Double Bond of the alpha,beta-unsaturated ketone is important for biological activity, while the 6-hydroxy and 30-carboxy group can tolerate a variety of modifications. The importance of the 9,10 Carbon-Carbon Double Bond was confirmed by the traditional growth inhibition assay. The high potency of 2 as an inducer of apoptosis, its novel mechanism of action, easy isolation and abundant supply, as well as the fact that it is amenable to chemical modification, makes gambogic acid an attractive molecule for the development of anticancer agents.