The Experts below are selected from a list of 327 Experts worldwide ranked by ideXlab platform
Bartolo Gabriele - One of the best experts on this subject based on the ideXlab platform.
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divergent multicomponent tandem palladium catalyzed aminocarbonylation cyclization approaches to functionalized imidazothiazinones and Imidazothiazoles
Chemcatchem, 2015Co-Authors: Lucia Veltri, Raffaella Mancuso, Angela Altomare, Bartolo GabrieleAbstract:The reactivity of 2-(prop-2-ynylthio)imidazoles under PdI2/KI-catalyzed oxidative aminocarbonylation conditions has been studied. Under relatively mild conditions, 0.33–1 mol % of catalyst at 100 °C in MeCN and under 20 atm (at 25 °C) of a 4:1 mixture of CO/air, and in the presence of an equimolar amount of a secondary nucleophilic amine, substrates that are unsubstituted or bear a single substituent on the imidazole ring were converted directly in a multicomponent fashion into functionalized imidazothiazinones. This transformation occurred through a new auto-tandem catalysis process that involves two concatenated catalytic cycles both catalyzed by PdI2: oxidative aminocarbonylation of the terminal triple bond/cyclocarbonylation. However, in the presence of an excess of secondary amine, 4,5-disubstituted substrates led selectively to functionalized Imidazothiazoles through an oxidative aminocarbonylation/conjugate addition process.
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Divergent Multicomponent Tandem Palladium‐Catalyzed Aminocarbonylation‐Cyclization Approaches to Functionalized Imidazothiazinones and Imidazothiazoles
Chemcatchem, 2015Co-Authors: Lucia Veltri, Raffaella Mancuso, Angela Altomare, Bartolo GabrieleAbstract:The reactivity of 2-(prop-2-ynylthio)imidazoles under PdI2/KI-catalyzed oxidative aminocarbonylation conditions has been studied. Under relatively mild conditions, 0.33–1 mol % of catalyst at 100 °C in MeCN and under 20 atm (at 25 °C) of a 4:1 mixture of CO/air, and in the presence of an equimolar amount of a secondary nucleophilic amine, substrates that are unsubstituted or bear a single substituent on the imidazole ring were converted directly in a multicomponent fashion into functionalized imidazothiazinones. This transformation occurred through a new auto-tandem catalysis process that involves two concatenated catalytic cycles both catalyzed by PdI2: oxidative aminocarbonylation of the terminal triple bond/cyclocarbonylation. However, in the presence of an excess of secondary amine, 4,5-disubstituted substrates led selectively to functionalized Imidazothiazoles through an oxidative aminocarbonylation/conjugate addition process.
Lucia Veltri - One of the best experts on this subject based on the ideXlab platform.
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divergent multicomponent tandem palladium catalyzed aminocarbonylation cyclization approaches to functionalized imidazothiazinones and Imidazothiazoles
Chemcatchem, 2015Co-Authors: Lucia Veltri, Raffaella Mancuso, Angela Altomare, Bartolo GabrieleAbstract:The reactivity of 2-(prop-2-ynylthio)imidazoles under PdI2/KI-catalyzed oxidative aminocarbonylation conditions has been studied. Under relatively mild conditions, 0.33–1 mol % of catalyst at 100 °C in MeCN and under 20 atm (at 25 °C) of a 4:1 mixture of CO/air, and in the presence of an equimolar amount of a secondary nucleophilic amine, substrates that are unsubstituted or bear a single substituent on the imidazole ring were converted directly in a multicomponent fashion into functionalized imidazothiazinones. This transformation occurred through a new auto-tandem catalysis process that involves two concatenated catalytic cycles both catalyzed by PdI2: oxidative aminocarbonylation of the terminal triple bond/cyclocarbonylation. However, in the presence of an excess of secondary amine, 4,5-disubstituted substrates led selectively to functionalized Imidazothiazoles through an oxidative aminocarbonylation/conjugate addition process.
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Divergent Multicomponent Tandem Palladium‐Catalyzed Aminocarbonylation‐Cyclization Approaches to Functionalized Imidazothiazinones and Imidazothiazoles
Chemcatchem, 2015Co-Authors: Lucia Veltri, Raffaella Mancuso, Angela Altomare, Bartolo GabrieleAbstract:The reactivity of 2-(prop-2-ynylthio)imidazoles under PdI2/KI-catalyzed oxidative aminocarbonylation conditions has been studied. Under relatively mild conditions, 0.33–1 mol % of catalyst at 100 °C in MeCN and under 20 atm (at 25 °C) of a 4:1 mixture of CO/air, and in the presence of an equimolar amount of a secondary nucleophilic amine, substrates that are unsubstituted or bear a single substituent on the imidazole ring were converted directly in a multicomponent fashion into functionalized imidazothiazinones. This transformation occurred through a new auto-tandem catalysis process that involves two concatenated catalytic cycles both catalyzed by PdI2: oxidative aminocarbonylation of the terminal triple bond/cyclocarbonylation. However, in the presence of an excess of secondary amine, 4,5-disubstituted substrates led selectively to functionalized Imidazothiazoles through an oxidative aminocarbonylation/conjugate addition process.
Angela Altomare - One of the best experts on this subject based on the ideXlab platform.
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divergent multicomponent tandem palladium catalyzed aminocarbonylation cyclization approaches to functionalized imidazothiazinones and Imidazothiazoles
Chemcatchem, 2015Co-Authors: Lucia Veltri, Raffaella Mancuso, Angela Altomare, Bartolo GabrieleAbstract:The reactivity of 2-(prop-2-ynylthio)imidazoles under PdI2/KI-catalyzed oxidative aminocarbonylation conditions has been studied. Under relatively mild conditions, 0.33–1 mol % of catalyst at 100 °C in MeCN and under 20 atm (at 25 °C) of a 4:1 mixture of CO/air, and in the presence of an equimolar amount of a secondary nucleophilic amine, substrates that are unsubstituted or bear a single substituent on the imidazole ring were converted directly in a multicomponent fashion into functionalized imidazothiazinones. This transformation occurred through a new auto-tandem catalysis process that involves two concatenated catalytic cycles both catalyzed by PdI2: oxidative aminocarbonylation of the terminal triple bond/cyclocarbonylation. However, in the presence of an excess of secondary amine, 4,5-disubstituted substrates led selectively to functionalized Imidazothiazoles through an oxidative aminocarbonylation/conjugate addition process.
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Divergent Multicomponent Tandem Palladium‐Catalyzed Aminocarbonylation‐Cyclization Approaches to Functionalized Imidazothiazinones and Imidazothiazoles
Chemcatchem, 2015Co-Authors: Lucia Veltri, Raffaella Mancuso, Angela Altomare, Bartolo GabrieleAbstract:The reactivity of 2-(prop-2-ynylthio)imidazoles under PdI2/KI-catalyzed oxidative aminocarbonylation conditions has been studied. Under relatively mild conditions, 0.33–1 mol % of catalyst at 100 °C in MeCN and under 20 atm (at 25 °C) of a 4:1 mixture of CO/air, and in the presence of an equimolar amount of a secondary nucleophilic amine, substrates that are unsubstituted or bear a single substituent on the imidazole ring were converted directly in a multicomponent fashion into functionalized imidazothiazinones. This transformation occurred through a new auto-tandem catalysis process that involves two concatenated catalytic cycles both catalyzed by PdI2: oxidative aminocarbonylation of the terminal triple bond/cyclocarbonylation. However, in the presence of an excess of secondary amine, 4,5-disubstituted substrates led selectively to functionalized Imidazothiazoles through an oxidative aminocarbonylation/conjugate addition process.
Raffaella Mancuso - One of the best experts on this subject based on the ideXlab platform.
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divergent multicomponent tandem palladium catalyzed aminocarbonylation cyclization approaches to functionalized imidazothiazinones and Imidazothiazoles
Chemcatchem, 2015Co-Authors: Lucia Veltri, Raffaella Mancuso, Angela Altomare, Bartolo GabrieleAbstract:The reactivity of 2-(prop-2-ynylthio)imidazoles under PdI2/KI-catalyzed oxidative aminocarbonylation conditions has been studied. Under relatively mild conditions, 0.33–1 mol % of catalyst at 100 °C in MeCN and under 20 atm (at 25 °C) of a 4:1 mixture of CO/air, and in the presence of an equimolar amount of a secondary nucleophilic amine, substrates that are unsubstituted or bear a single substituent on the imidazole ring were converted directly in a multicomponent fashion into functionalized imidazothiazinones. This transformation occurred through a new auto-tandem catalysis process that involves two concatenated catalytic cycles both catalyzed by PdI2: oxidative aminocarbonylation of the terminal triple bond/cyclocarbonylation. However, in the presence of an excess of secondary amine, 4,5-disubstituted substrates led selectively to functionalized Imidazothiazoles through an oxidative aminocarbonylation/conjugate addition process.
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Divergent Multicomponent Tandem Palladium‐Catalyzed Aminocarbonylation‐Cyclization Approaches to Functionalized Imidazothiazinones and Imidazothiazoles
Chemcatchem, 2015Co-Authors: Lucia Veltri, Raffaella Mancuso, Angela Altomare, Bartolo GabrieleAbstract:The reactivity of 2-(prop-2-ynylthio)imidazoles under PdI2/KI-catalyzed oxidative aminocarbonylation conditions has been studied. Under relatively mild conditions, 0.33–1 mol % of catalyst at 100 °C in MeCN and under 20 atm (at 25 °C) of a 4:1 mixture of CO/air, and in the presence of an equimolar amount of a secondary nucleophilic amine, substrates that are unsubstituted or bear a single substituent on the imidazole ring were converted directly in a multicomponent fashion into functionalized imidazothiazinones. This transformation occurred through a new auto-tandem catalysis process that involves two concatenated catalytic cycles both catalyzed by PdI2: oxidative aminocarbonylation of the terminal triple bond/cyclocarbonylation. However, in the presence of an excess of secondary amine, 4,5-disubstituted substrates led selectively to functionalized Imidazothiazoles through an oxidative aminocarbonylation/conjugate addition process.
Ahmed Kamal - One of the best experts on this subject based on the ideXlab platform.
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development and biological evaluation of Imidazothiazole propenones as tubulin inhibitors that effectively triggered apoptotic cell death in alveolar lung cancer cell line
ChemistrySelect, 2017Co-Authors: Ahmed Kamal, Ibrahim Bin Sayeed, Koteswara Rao Garikapati, Venkata Krishna Kanth Makani, Apoorva Nagarajan, Mohd Adil Shareef, Abdallah Alarifi, Manika PalbhadraAbstract:A new class of Imidazothiazole-propenones was synthesized and investigated for their anti-proliferative activity against various human cancer cell lines. Promising activities were observed in five congeners 8 k, 8 l, 8 n, 8 o and 8 v with interesting cytotoxicity profiles. The detailed biological aspects of these congeners towards human lung cancer cell line (A549) were studied. Cell cycle assay revealed that these molecules arrested cell growth in G2/M phase of the cell cycle in a concentration-dependent manner and lead to apoptotic cell death, confirmed by caspase-3 activation assay. Further, the tubulin polymerization inhibition analysis results suggested that these congeners exhibited significant inhibitory effect on the tubulin assembly. Western blotting displayed that pro-apoptotic proteins were markedly up regulated resulting in apoptosis. The investigations displayed that such congeners containing Imidazothiazole-propenone have the potential in the development of newer chemotherapeutic agents.
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the design and development of Imidazothiazole chalcone derivatives as potential anticancer drugs
Expert Opinion on Drug Discovery, 2013Co-Authors: Ahmed Kamal, Methuku Kashi Reddy, A ViswanathAbstract:Introduction: Imidazothiazole derivatives have long been therapeutically used for the treatment of various diseases. In recent years, the Imidazothiazole and chalcone moieties have emerged as important pharmacophores in the development of antitumor agents. Imidazothiazole–chalcone conjugates can be accessed by covalently binding these two powerful pharamacophore units. These conjugates are known to exhibit a wide range of biological properties, including anticancer, antimicrobial, anti-inflammatory and immunosuppressive activities. Their promising biological profile and easy synthetic accessibility have triggered investigations directed at the design and development of new Imidazothiazole–chalcone conjugate derivatives as potential chemotherapeutics. Areas covered: The present review focuses on recent reports of the syntheses and anticancer properties of various Imidazothiazoles, chalcones and Imidazothiazole-linked chalcone conjugates. Furthermore, the authors discuss the structure–activity relationships...
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The design and development of Imidazothiazole–chalcone derivatives as potential anticancer drugs
Expert Opinion on Drug Discovery, 2013Co-Authors: Ahmed Kamal, Methuku Kashi Reddy, A ViswanathAbstract:Introduction: Imidazothiazole derivatives have long been therapeutically used for the treatment of various diseases. In recent years, the Imidazothiazole and chalcone moieties have emerged as important pharmacophores in the development of antitumor agents. Imidazothiazole–chalcone conjugates can be accessed by covalently binding these two powerful pharamacophore units. These conjugates are known to exhibit a wide range of biological properties, including anticancer, antimicrobial, anti-inflammatory and immunosuppressive activities. Their promising biological profile and easy synthetic accessibility have triggered investigations directed at the design and development of new Imidazothiazole–chalcone conjugate derivatives as potential chemotherapeutics. Areas covered: The present review focuses on recent reports of the syntheses and anticancer properties of various Imidazothiazoles, chalcones and Imidazothiazole-linked chalcone conjugates. Furthermore, the authors discuss the structure–activity relationships...
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synthesis of Imidazothiazole chalcone derivatives as anticancer and apoptosis inducing agents
ChemMedChem, 2010Co-Authors: Ahmed Kamal, D Dastagiri, Janaki M Ramaiah, Surendranadha J Reddy, Vijaya E Bharathi, Chatla Srinivas, S N C V L Pushpavalli, Manika PalbhadraAbstract:A new class of imidazo[2,1-b]thiazole chalcone derivatives were synthesized and evaluated for their anticancer activity. These chalcone derivatives show promising activity, with log GI50 values ranging from −7.51 to −4.00. The detailed biological aspects of these derivatives toward the MCF-7 cell line were studied. Interestingly, these chalcone derivatives induced G0/G1-phase cell-cycle arrest, down-regulation of G1-phase cell-cycle regulatory proteins such as cyclin D1 and cyclin E1, and up-regulation of CDK4. Moreover, these compounds elicit the characteristic features of apoptosis such as enhancement in the levels of p53, p21, and p27, suppression of NF-κB, and up-regulation of caspase-9. One of these chalcone derivatives, 3 d, is potentially well suited for detailed biological studies, either alone or in combination with existing therapies.
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Synthesis of Imidazothiazole–Chalcone Derivatives as Anticancer and Apoptosis Inducing Agents
ChemMedChem, 2010Co-Authors: Ahmed Kamal, D Dastagiri, Chatla Srinivas, S N C V L Pushpavalli, M. Janaki Ramaiah, J. Surendranadha Reddy, E. Vijaya Bharathi, Manika Pal-bhadraAbstract:A new class of imidazo[2,1-b]thiazole chalcone derivatives were synthesized and evaluated for their anticancer activity. These chalcone derivatives show promising activity, with log GI50 values ranging from −7.51 to −4.00. The detailed biological aspects of these derivatives toward the MCF-7 cell line were studied. Interestingly, these chalcone derivatives induced G0/G1-phase cell-cycle arrest, down-regulation of G1-phase cell-cycle regulatory proteins such as cyclin D1 and cyclin E1, and up-regulation of CDK4. Moreover, these compounds elicit the characteristic features of apoptosis such as enhancement in the levels of p53, p21, and p27, suppression of NF-κB, and up-regulation of caspase-9. One of these chalcone derivatives, 3 d, is potentially well suited for detailed biological studies, either alone or in combination with existing therapies.
