Category: 252932-48-2

Zheng, Youguang; Wu, Xiaoqing; Sun, Min; Feng, Liuhai; Li, Mingdong; Ji, Min published the artcile< Design, synthesis, crystal structure and antitumor activity of a new ethyl 3-(quinazolin-4-ylamino)-1H-pyrrole-2-carboxylate derivative>, Category: esters-buliding-blocks, the main research area is pyrrolecarboxylate quinazolinylamino morpholinopropoxy methoxy preparation antitumor activity crystal structure.

A new Et 3-(quinazolin-4-ylamino)-1H-pyrrole-2-carboxylate derivative I was designed and synthesized as an antitumor agent. The antitumor activity of the new compound was tested against human pancreatic cancer Miacapa2, pancreatic cancer Panc1, prostate cancer DU145 and prostate cancer PC3 cells in vitro. The crystal structure of I was characterized by x-ray crystal anal.

Letters in Drug Design & Discovery published new progress about Antitumor agents. 252932-48-2 belongs to class esters-buliding-blocks, and the molecular formula is C7H10N2O2, Category: esters-buliding-blocks.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Zhang, Ying-Qi; Zhang, Yi-Ping; Zheng, Yan-Xin; Li, Zhao-Yang; Ye, Long-Wu published the artcile< Rapid and practical access to diverse quindolines by catalyst-free and regioselectivity-reversed Povarov reaction>, Quality Control of 252932-48-2, the main research area is quindoline preparation regioselective; arylimine dienophile Povarov reaction.

The Povarov reaction, a formal [4 + 2] cycloaddition between N-aryl imines and electron-rich dienophiles, has been defined as an efficient method to approach tetrahydroquinolines and has been well established in the past decades. In general, electron-rich heterosubstituted alkenes have served as the most popular dienophiles to achieve the exclusive regioselectivity. However, the use of Lewis acids and Bronsted acids as catalysts is required in these transformations, and, to authors knowledge, the Povarov reaction of electron-rich heterosubstituted alkynes has not been reported. Here, authors disclose a catalyst-free Povarov reaction of formyl-ynamides with anilines for the rapid and practical synthesis of a diverse range of valuable quindolines, which not only represents the first Povarov reaction of ynamides to the best of authors knowledge but also constitutes a very rare example of a catalyst-free ynamide cyclization reaction. This formal [1 + 2 + 3] annulation shows a reversed regioselectivity compared with the previous protocols.

Cell Reports Physical Science published new progress about [4+2] Cycloaddition reaction. 252932-48-2 belongs to class esters-buliding-blocks, and the molecular formula is C7H10N2O2, Quality Control of 252932-48-2.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Furneaux, Richard H.; Tyler, Peter C. published the artcile< Improved Syntheses of 3H,5H-Pyrrolo[3,2-d]pyrimidines>, Computed Properties of 252932-48-2, the main research area is pyrrolopyrimidine preparation; pyrrolopyrimidinone deazaguanine triazaindenone preparation; aminopyrrolopyrimidinone deazahypoxanthine preparation.

A convenient, direct synthetic routes for the preparation of 9-deazahypoxanthine (1,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one) and 9-deazaguanine (2-amino-1,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one) were developed.

Journal of Organic Chemistry published new progress about 252932-48-2. 252932-48-2 belongs to class esters-buliding-blocks, and the molecular formula is C7H10N2O2, Computed Properties of 252932-48-2.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Mirguet, Olivier; Sautet, Stephane; Clement, Catherine-Anne; Toum, Jerome; Donche, Frederic; Marques, Celine; Rondet, Emilie; Pizzonero, Mathieu; Beaufils, Benjamin; Dudit, Yann; Huet, Pascal; Trottet, Lionel; Grondin, Pascal; Brusq, Jean-Marie; Boursier, Eric; Saintillan, Yannick; Nicodeme, Edwige published the artcile< Discovery of Pyridones as Oral AMPK Direct Activators>, Recommanded Product: Ethyl 3-amino-1H-pyrrole-2-carboxylate, the main research area is pyridone AMPK activator diabetes type 2 structure activity preperation; AMPK direct activator; P-gp substrate; pyridone; type 2 diabetes.

AMP-activated protein kinase (AMPK) is an evolutionarily conserved fuel-sensing enzyme that is activated in shortage of energy and suppressed in its surfeit. AMPK activation stimulates fatty acid oxidation, enhances insulin sensitivity, alleviates hyperglycemia and hyperlipidemia, and inhibits proinflammatory changes. Thus, AMPK is a well-received therapeutic target for type 2 diabetes and other metabolic disorders. Here, the authors will report the discovery of pyrrolopyridone derivatives as AMPK direct activators. The authors will illustrate the synthesis and structure-activity relationships of the series as well as some pharmacokinetic results. Some compounds exhibited encouraging oral exposure and were evaluated in a mouse diabetic model. 2-Chloro-7-hydroxy-1-[2′-hydroxy-3′-(methyloxy)-4-biphenylyl]-6-phenyl-1,4-dihydro5H-pyrrolo[3,2-b]pyridin-5-one showed oral activity at 30 mg/kg on blood glucose.

ACS Medicinal Chemistry Letters published new progress about Drug discovery. 252932-48-2 belongs to class esters-buliding-blocks, and the molecular formula is C7H10N2O2, Recommanded Product: Ethyl 3-amino-1H-pyrrole-2-carboxylate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Malcor, Jean-Daniel; Brouillette, Yann; Graffion, Julien; Spielmann, Kim; Masurier, Nicolas; Maillard, Ludovic T.; Martinez, Jean; Lisowski, Vincent published the artcile< Synthesis and reactivity of pyrrolo[3,2-d][1,3]oxazine-2,4-dione. Access to new pyrrolo[3,2-e][1,4]diazepine-2,5-diones>, Safety of Ethyl 3-amino-1H-pyrrole-2-carboxylate, the main research area is pyrrolodiazepinedione preparation nucleophile reactivity.

A convenient synthesis of pyrrolo[3,2-d][1,3]oxazine-2,4-dione is described and its reactivity towards various nucleophiles studied. The regioselective ring opening of pyrrolo[3,2-d][1,3]oxazine-2,4-dione or its N-alkylated analog in the presence of alanine or proline afforded, resp., imidazolidinedione and 2 N-protected pyrrolo[3,2-e][1,4]diazepines in a one-pot process. In a last part of this study, an alternative route to produce a library of eight non protected pyrrolo[3,2-e][1,4]diazepine-2,5-diones is described to overcome the limited reactivity of pyrrolo[3,2-d][1,3]oxazine-2,4-dione.

Tetrahedron published new progress about Nucleophiles. 252932-48-2 belongs to class esters-buliding-blocks, and the molecular formula is C7H10N2O2, Safety of Ethyl 3-amino-1H-pyrrole-2-carboxylate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Mingoia, Francesco published the artcile< Reactivity of 5-(3-azidophenyl)-1-(1H-pyrrol-3-yl)pyrroles in TFMSA. A route for new ring systems as DNA-interactive agents>, Formula: C7H10N2O2, the main research area is azidophenyl pyrrolylpyrrole preparation cyclization; dipyrroloisoquinoline preparation DNA interactive agent.

Acid catalyzed decomposition of 5-(3-azidophenyl)-1-(1H-pyrrol-3-yl)pyrroles did not afford the expected dipyrrolo[2,1-a:3,4-c]isoquinoline derivatives, but the planar dipyrrolo[2,1-a:3,2-c]isoquinoline derivatives and related non planar derivatives H-dipyrrolo[2,1-a:3,2-c]isoquinoline derivatives In strong acid media (trifluoromethanesulfonic acid) the α-(1-pyrrol-3-yl) position even if blocked, was more prone to undergo cyclization with respect to the free β one. Despite the steric hindrance, these compounds were obtained in moderate to good overall yields, depending on the nature and position of the substituents on the 1-(1H-pyrrolyl) moiety.

Tetrahedron published new progress about DNA Role: MSC (Miscellaneous). 252932-48-2 belongs to class esters-buliding-blocks, and the molecular formula is C7H10N2O2, Formula: C7H10N2O2.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Carry, Jean-Christophe; Clerc, Francois; Minoux, Herve; Schio, Laurent; Mauger, Jacques; Nair, Anil; Parmantier, Eric; Le Moigne, Ronan; Delorme, Cecile; Nicolas, Jean-Paul; Krick, Alain; Abecassis, Pierre-Yves; Crocq-Stuerga, Veronique; Pouzieux, Stephanie; Delarbre, Laure; Maignan, Sebastien; Bertrand, Thomas; Bjergarde, Kirsten; Ma, Nina; Lachaud, Sylvette; Guizani, Houlfa; Lebel, Remi; Doerflinger, Gilles; Monget, Sylvie; Perron, Sebastien; Gasse, Francis; Angouillant-Boniface, Odile; Filoche-Romme, Bruno; Murer, Michel; Gontier, Sylvie; Prevost, Celine; Monteiro, Marie-Line; Combeau, Cecile published the artcile< SAR156497, an Exquisitely Selective Inhibitor of Aurora Kinases>, Related Products of 252932-48-2, the main research area is SAR156497 antitumor Aurora kinase.

The Aurora family of serine/threonine kinases is essential for mitosis. Their crucial role in cell cycle regulation and aberrant expression in a broad range of malignancies have been demonstrated and have prompted intensive search for small mol. Aurora inhibitors. Indeed, over 10 of them have reached the clinic as potential anticancer therapies. We report herein the discovery and optimization of a novel series of tricyclic mols. that has led to SAR156497, an exquisitely selective Aurora A, B, and C inhibitor with in vitro and in vivo efficacy. We also provide insights into its mode of binding to its target proteins, which could explain its selectivity.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 252932-48-2 belongs to class esters-buliding-blocks, and the molecular formula is C7H10N2O2, Related Products of 252932-48-2.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Wang, Shengzheng; Fang, Kun; Dong, Guoqiang; Chen, Shuqiang; Liu, Na; Miao, Zhenyuan; Yao, Jianzhong; Li, Jian; Zhang, Wannian; Sheng, Chunquan published the artcile< Scaffold diversity inspired by the natural product evodiamine: discovery of highly potent and multitargeting antitumor agents>, Recommanded Product: Ethyl 3-amino-1H-pyrrole-2-carboxylate, the main research area is evodiamine scaffold antitumor neoplasm.

A critical question in natural product-based drug discovery is how to translate the product into drug-like mols. with optimal pharmacol. properties. The generation of natural product-inspired scaffold diversity is an effective but challenging strategy to investigate the broader chem. space and identify promising drug leads. Extending the efforts to the natural product evodiamine, a diverse library containing 11 evodiamine-inspired novel scaffolds and their derivatives were designed and synthesized. Most of them showed good to excellent antitumor activity against various human cancer cell lines. In particular, 3-chloro-10-hydroxyl thio-evodiamine I showed excellent in vitro and in vivo antitumor efficacy with good tolerability and low toxicity. Antitumor mechanism and target profiling studies indicate that compound I is the first-in-class triple topoisomerase I/topoisomerase II/tubulin inhibitor. Overall, this study provided an effective strategy for natural product-based drug discovery.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 252932-48-2 belongs to class esters-buliding-blocks, and the molecular formula is C7H10N2O2, Recommanded Product: Ethyl 3-amino-1H-pyrrole-2-carboxylate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Carry, Jean-Christophe; Clerc, Francois; Minoux, Herve; Schio, Laurent; Mauger, Jacques; Nair, Anil; Parmantier, Eric; Le Moigne, Ronan; Delorme, Cecile; Nicolas, Jean-Paul; Krick, Alain; Abecassis, Pierre-Yves; Crocq-Stuerga, Veronique; Pouzieux, Stephanie; Delarbre, Laure; Maignan, Sebastien; Bertrand, Thomas; Bjergarde, Kirsten; Ma, Nina; Lachaud, Sylvette; Guizani, Houlfa; Lebel, Remi; Doerflinger, Gilles; Monget, Sylvie; Perron, Sebastien; Gasse, Francis; Angouillant-Boniface, Odile; Filoche-Romme, Bruno; Murer, Michel; Gontier, Sylvie; Prevost, Celine; Monteiro, Marie-Line; Combeau, Cecile published the artcile< SAR156497, an Exquisitely Selective Inhibitor of Aurora Kinases>, Related Products of 252932-48-2, the main research area is SAR156497 antitumor Aurora kinase.

The Aurora family of serine/threonine kinases is essential for mitosis. Their crucial role in cell cycle regulation and aberrant expression in a broad range of malignancies have been demonstrated and have prompted intensive search for small mol. Aurora inhibitors. Indeed, over 10 of them have reached the clinic as potential anticancer therapies. We report herein the discovery and optimization of a novel series of tricyclic mols. that has led to SAR156497, an exquisitely selective Aurora A, B, and C inhibitor with in vitro and in vivo efficacy. We also provide insights into its mode of binding to its target proteins, which could explain its selectivity.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 252932-48-2 belongs to class esters-buliding-blocks, and the molecular formula is C7H10N2O2, Related Products of 252932-48-2.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Wang, Shengzheng; Fang, Kun; Dong, Guoqiang; Chen, Shuqiang; Liu, Na; Miao, Zhenyuan; Yao, Jianzhong; Li, Jian; Zhang, Wannian; Sheng, Chunquan published the artcile< Scaffold diversity inspired by the natural product evodiamine: discovery of highly potent and multitargeting antitumor agents>, Recommanded Product: Ethyl 3-amino-1H-pyrrole-2-carboxylate, the main research area is evodiamine scaffold antitumor neoplasm.

A critical question in natural product-based drug discovery is how to translate the product into drug-like mols. with optimal pharmacol. properties. The generation of natural product-inspired scaffold diversity is an effective but challenging strategy to investigate the broader chem. space and identify promising drug leads. Extending the efforts to the natural product evodiamine, a diverse library containing 11 evodiamine-inspired novel scaffolds and their derivatives were designed and synthesized. Most of them showed good to excellent antitumor activity against various human cancer cell lines. In particular, 3-chloro-10-hydroxyl thio-evodiamine I showed excellent in vitro and in vivo antitumor efficacy with good tolerability and low toxicity. Antitumor mechanism and target profiling studies indicate that compound I is the first-in-class triple topoisomerase I/topoisomerase II/tubulin inhibitor. Overall, this study provided an effective strategy for natural product-based drug discovery.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 252932-48-2 belongs to class esters-buliding-blocks, and the molecular formula is C7H10N2O2, Recommanded Product: Ethyl 3-amino-1H-pyrrole-2-carboxylate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics