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Anna Maria Almerico - One of the best experts on this subject based on the ideXlab platform.
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An Unexpected Dimroth Rearrangement Leading to Anellated Thieno[3,2‐d][1,2,3]triazolo[1,5‐a]pyrimidines with Potent Antitumor Activity.
ChemInform, 2013Co-Authors: Antonino Lauria, Chiara Patella, Ilenia Abbate, Annamaria Martorana, Anna Maria AlmericoAbstract:Compounds (I) undergo an unexpected Dimroth Rearrangement under basic conditions to give mainly the linear fused isomers (III).
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An unexpected Dimroth Rearrangement leading to annelated thieno[3,2-d][1,2,3]triazolo[1,5-a]pyrimidines with potent antitumor activity.
European journal of medicinal chemistry, 2013Co-Authors: Antonino Lauria, Chiara Patella, Ilenia Abbate, Annamaria Martorana, Anna Maria AlmericoAbstract:An unusual Dimroth Rearrangement occurring in the reaction leading to annelated thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidine core allowed the isolation of the linear isomer thieno[3,2-d][1,2,3]triazolo[1,5-a]pyrimidine. By decorating the linear isomer with the same chains that improved the biological activity of the angular isomers, new annelated thieno[3,2-d][1,2,3]triazolo[1,5-a]pyrimidines were designed and synthesized. They were selected by the Developmental Therapeutics Program (DTP) of the National Cancer Institute (NCI) for the anticancer screening against a panel of 60 human tumor cell lines. The biological results showed that the new derivatives exhibited strong antiproliferative activity up to nanomolar concentration. In vivo screenings of the most active compound, the N-[2-(1H-imidazol-4-yl)ethyl]-4-(3-phenyl-10-oxo-4,10-dihydrobenzothieno[3,2-d][1,2,3]triazolo[1,5-a]pyrimidin-4-yl)butanamide, showed its low toxicity and high potency.
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Pyrazolo[3,4-d][1,2,3]triazolo[1,5-a]pyrimidine: a new ring system through Dimroth Rearrangement
Tetrahedron Letters, 2008Co-Authors: Antonino Lauria, Chiara Patella, Ilenia Abbate, Noemi Gambino, Arturo Silvestri, Giampaolo Barone, Anna Maria AlmericoAbstract:Abstract Derivatives of the new ring system pyrazolo[3,4- d ][1,2,3]triazolo[1,5- a ]pyrimidine were synthesized from the corresponding angular isomers, through a Dimroth Rearrangement, in quantitative yields. Preliminary computational studies demonstrated that this class of compounds could be a good candidate as DNA intercalating agents.
Antonino Lauria - One of the best experts on this subject based on the ideXlab platform.
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An Unexpected Dimroth Rearrangement Leading to Anellated Thieno[3,2‐d][1,2,3]triazolo[1,5‐a]pyrimidines with Potent Antitumor Activity.
ChemInform, 2013Co-Authors: Antonino Lauria, Chiara Patella, Ilenia Abbate, Annamaria Martorana, Anna Maria AlmericoAbstract:Compounds (I) undergo an unexpected Dimroth Rearrangement under basic conditions to give mainly the linear fused isomers (III).
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An unexpected Dimroth Rearrangement leading to annelated thieno[3,2-d][1,2,3]triazolo[1,5-a]pyrimidines with potent antitumor activity.
European journal of medicinal chemistry, 2013Co-Authors: Antonino Lauria, Chiara Patella, Ilenia Abbate, Annamaria Martorana, Anna Maria AlmericoAbstract:An unusual Dimroth Rearrangement occurring in the reaction leading to annelated thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidine core allowed the isolation of the linear isomer thieno[3,2-d][1,2,3]triazolo[1,5-a]pyrimidine. By decorating the linear isomer with the same chains that improved the biological activity of the angular isomers, new annelated thieno[3,2-d][1,2,3]triazolo[1,5-a]pyrimidines were designed and synthesized. They were selected by the Developmental Therapeutics Program (DTP) of the National Cancer Institute (NCI) for the anticancer screening against a panel of 60 human tumor cell lines. The biological results showed that the new derivatives exhibited strong antiproliferative activity up to nanomolar concentration. In vivo screenings of the most active compound, the N-[2-(1H-imidazol-4-yl)ethyl]-4-(3-phenyl-10-oxo-4,10-dihydrobenzothieno[3,2-d][1,2,3]triazolo[1,5-a]pyrimidin-4-yl)butanamide, showed its low toxicity and high potency.
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Pyrazolo[3,4-d][1,2,3]triazolo[1,5-a]pyrimidine: a new ring system through Dimroth Rearrangement
Tetrahedron Letters, 2008Co-Authors: Antonino Lauria, Chiara Patella, Ilenia Abbate, Noemi Gambino, Arturo Silvestri, Giampaolo Barone, Anna Maria AlmericoAbstract:Abstract Derivatives of the new ring system pyrazolo[3,4- d ][1,2,3]triazolo[1,5- a ]pyrimidine were synthesized from the corresponding angular isomers, through a Dimroth Rearrangement, in quantitative yields. Preliminary computational studies demonstrated that this class of compounds could be a good candidate as DNA intercalating agents.
Shi-fen Jiang - One of the best experts on this subject based on the ideXlab platform.
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A concise construction of 12H-benzo[4,5]thiazolo[2,3-b]quinazolin-12-ones via an unusual TBHP/Na2CO3 promoted cascade oxidative cyclization and interrupted Dimroth Rearrangement.
Chemical communications (Cambridge England), 2017Co-Authors: Zhi-wen Zhou, Feng-cheng Jia, Shi-fen JiangAbstract:An efficient transition-metal-free cascade reaction has been developed for the facile synthesis of 12H-benzo[4,5]thiazolo[2,3-b]quinazolin-12-one derivatives from commercially available isatins and 2-haloaryl isothiocyanates. A preliminary mechanistic study suggested an interrupted Dimroth Rearrangement was the key step for the successful transformation.
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a concise construction of 12h benzo 4 5 thiazolo 2 3 b quinazolin 12 ones via an unusual tbhp na2co3 promoted cascade oxidative cyclization and interrupted Dimroth Rearrangement
Chemical Communications, 2017Co-Authors: Zhi-wen Zhou, Feng-cheng Jia, Shi-fen JiangAbstract:An efficient transition-metal-free cascade reaction has been developed for the facile synthesis of 12H-benzo[4,5]thiazolo[2,3-b]quinazolin-12-one derivatives from commercially available isatins and 2-haloaryl isothiocyanates. A preliminary mechanistic study suggested an interrupted Dimroth Rearrangement was the key step for the successful transformation.
Chiara Patella - One of the best experts on this subject based on the ideXlab platform.
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An Unexpected Dimroth Rearrangement Leading to Anellated Thieno[3,2‐d][1,2,3]triazolo[1,5‐a]pyrimidines with Potent Antitumor Activity.
ChemInform, 2013Co-Authors: Antonino Lauria, Chiara Patella, Ilenia Abbate, Annamaria Martorana, Anna Maria AlmericoAbstract:Compounds (I) undergo an unexpected Dimroth Rearrangement under basic conditions to give mainly the linear fused isomers (III).
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An unexpected Dimroth Rearrangement leading to annelated thieno[3,2-d][1,2,3]triazolo[1,5-a]pyrimidines with potent antitumor activity.
European journal of medicinal chemistry, 2013Co-Authors: Antonino Lauria, Chiara Patella, Ilenia Abbate, Annamaria Martorana, Anna Maria AlmericoAbstract:An unusual Dimroth Rearrangement occurring in the reaction leading to annelated thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidine core allowed the isolation of the linear isomer thieno[3,2-d][1,2,3]triazolo[1,5-a]pyrimidine. By decorating the linear isomer with the same chains that improved the biological activity of the angular isomers, new annelated thieno[3,2-d][1,2,3]triazolo[1,5-a]pyrimidines were designed and synthesized. They were selected by the Developmental Therapeutics Program (DTP) of the National Cancer Institute (NCI) for the anticancer screening against a panel of 60 human tumor cell lines. The biological results showed that the new derivatives exhibited strong antiproliferative activity up to nanomolar concentration. In vivo screenings of the most active compound, the N-[2-(1H-imidazol-4-yl)ethyl]-4-(3-phenyl-10-oxo-4,10-dihydrobenzothieno[3,2-d][1,2,3]triazolo[1,5-a]pyrimidin-4-yl)butanamide, showed its low toxicity and high potency.
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Pyrazolo[3,4-d][1,2,3]triazolo[1,5-a]pyrimidine: a new ring system through Dimroth Rearrangement
Tetrahedron Letters, 2008Co-Authors: Antonino Lauria, Chiara Patella, Ilenia Abbate, Noemi Gambino, Arturo Silvestri, Giampaolo Barone, Anna Maria AlmericoAbstract:Abstract Derivatives of the new ring system pyrazolo[3,4- d ][1,2,3]triazolo[1,5- a ]pyrimidine were synthesized from the corresponding angular isomers, through a Dimroth Rearrangement, in quantitative yields. Preliminary computational studies demonstrated that this class of compounds could be a good candidate as DNA intercalating agents.
Ilenia Abbate - One of the best experts on this subject based on the ideXlab platform.
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An Unexpected Dimroth Rearrangement Leading to Anellated Thieno[3,2‐d][1,2,3]triazolo[1,5‐a]pyrimidines with Potent Antitumor Activity.
ChemInform, 2013Co-Authors: Antonino Lauria, Chiara Patella, Ilenia Abbate, Annamaria Martorana, Anna Maria AlmericoAbstract:Compounds (I) undergo an unexpected Dimroth Rearrangement under basic conditions to give mainly the linear fused isomers (III).
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An unexpected Dimroth Rearrangement leading to annelated thieno[3,2-d][1,2,3]triazolo[1,5-a]pyrimidines with potent antitumor activity.
European journal of medicinal chemistry, 2013Co-Authors: Antonino Lauria, Chiara Patella, Ilenia Abbate, Annamaria Martorana, Anna Maria AlmericoAbstract:An unusual Dimroth Rearrangement occurring in the reaction leading to annelated thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidine core allowed the isolation of the linear isomer thieno[3,2-d][1,2,3]triazolo[1,5-a]pyrimidine. By decorating the linear isomer with the same chains that improved the biological activity of the angular isomers, new annelated thieno[3,2-d][1,2,3]triazolo[1,5-a]pyrimidines were designed and synthesized. They were selected by the Developmental Therapeutics Program (DTP) of the National Cancer Institute (NCI) for the anticancer screening against a panel of 60 human tumor cell lines. The biological results showed that the new derivatives exhibited strong antiproliferative activity up to nanomolar concentration. In vivo screenings of the most active compound, the N-[2-(1H-imidazol-4-yl)ethyl]-4-(3-phenyl-10-oxo-4,10-dihydrobenzothieno[3,2-d][1,2,3]triazolo[1,5-a]pyrimidin-4-yl)butanamide, showed its low toxicity and high potency.
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Pyrazolo[3,4-d][1,2,3]triazolo[1,5-a]pyrimidine: a new ring system through Dimroth Rearrangement
Tetrahedron Letters, 2008Co-Authors: Antonino Lauria, Chiara Patella, Ilenia Abbate, Noemi Gambino, Arturo Silvestri, Giampaolo Barone, Anna Maria AlmericoAbstract:Abstract Derivatives of the new ring system pyrazolo[3,4- d ][1,2,3]triazolo[1,5- a ]pyrimidine were synthesized from the corresponding angular isomers, through a Dimroth Rearrangement, in quantitative yields. Preliminary computational studies demonstrated that this class of compounds could be a good candidate as DNA intercalating agents.