- Pyrrolopyrazoles: Synthesis, evaluation and pharmacological screening as antidepressant agents
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Background: Pyrroles and fused pyrroles are of great interest as biologically active compounds, among these activities; antidepressant activity is of special concern. Objective: Synthesis of a series of pyrrolopyrazoles and their pyrimidine derivatives an
- Abd El-hameed, Rania H.,Fatahala, Samar S.,Mahmoud, Eman,Nofal, Shahira
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p. 911 - 922
(2020/01/25)
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- Combination therapy for the inhibition of metastasis and tumorigenesis
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The invention provides therapeutic compositions and methods for the inhibition of metastasis and for treatment of cancers in human and non-human mammals that are directed to the coformulation and/or coadministration of a dehydropyrimidine dehydrogenase inhibitor such as gimeracil and a pyrrolopyrimidine compound.
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Page/Page column 23; 24
(2018/02/28)
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- Structure-activity relationship study and optimisation of 2-aminopyrrole-1-benzyl-4,5-diphenyl-1H-pyrrole-3-carbonitrile as a broad spectrum metallo-β-lactamase inhibitor
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A SAR study on derivatives of 2-amino-1-benzyl-4,5-diphenyl-1H-pyrrole-3-carbonitrile 5a revealed that the 3-carbonitrile group, vicinal 4,5-diphenyl and N-benzyl side chains of the pyrrole are important for the inhibitory potencies of these compounds against members representing the three main subclasses of metallo-β-lactamases (MBLs), i.e. IMP-1 (representing the B1 subgroup), CphA (B2) and AIM-1 (B3). Coupling of 5a with a series of acyl chlorides and anhydrides led to the discovery of two N-acylamide derivatives, 10 and 11, as the two most potent IMP-1 inhibitors in this series. However, these compounds are less effective towards CphA and AIM-1. The N-benzoyl derivative of 5a retained potent in vitro activity against each of MBLs tested (with inhibition constants in the low μM range). Importantly, this compound also significantly enhanced the sensitivity of IMP-1, CphA- or AIM-1-producing cell cultures towards meropenem. This compound presents a promising starting point for the development of a universal MBL inhibitor, targeting members of each of the major subgroups of this family of enzymes.
- McGeary, Ross P.,Tan, Daniel T.C.,Selleck, Christopher,Monteiro Pedroso, Marcelo,Sidjabat, Hanna E.,Schenk, Gerhard
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p. 351 - 364
(2017/06/19)
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- COMPOUNDS AND METHODS FOR THE PREVENTION AND TREATMENT OF TUMOR METASTASIS AND TUMORIGENESIS
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The disclosure provides compounds for reducing the prevalence of the perinucleolar compartment in cells, for example, of formula (I), wherein R1, R2, R3, and R4 are as defined herein, that are useful in treating a disease or disorder associated with increased prevalence of the perinucleolar compartment, such as cancer. Also disclosed is a composition containing a pharmaceutically acceptable carrier and at least one compound embodying the principles of the invention, and a method of treating or preventing cancer in a mammal.
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Paragraph 0093
(2013/07/05)
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- Identification, SAR studies, and X-ray Co-crystallographic analysis of a novel furanopyrimidine aurora kinase a inhibitor
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Herein we reveal a simple method for the identification of novel Aurora kinase A inhibitors through substructure searching of an in-house compound library to select compounds for testing. A hydrazone fragment conferring Aurora kinase activity and heterocy
- Coumar, Mohane Selvaraj,Tsai, Ming-Tsung,Chu, Chang-Ying,Uang, Biing-Jiun,Lin, Wen-Hsing,Chang, Chun-Yu,Chang, Teng-Yuan,Leou, Jiun-Shyang,Teng, Chi-Huang,Wu, Jian-Sung,Fang, Ming-Yu,Chen, Chun-Hwa,Hsu, John T.-A.,Wu, Su-Ying,Chao, Yu-Sheng,Hsieh, Hsing-Pang
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experimental part
p. 255 - 267
(2010/12/18)
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- Synthesis and rearrangements of 7H-pyrrolo[3,2-e][1,2,4]triazolo[1,5-c]-and 7h-pyrrolo[3,2-e][1,2,4]triazolo[4,3-c]pyrimidines
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7H-Pyrrolo[3,2-e][1,2,4]triazolo[1,5-c]pyrimidines were synthesized by the reactions of 2-ethoxymethyleneamino-1H-pyrrole-3-carbonitriles with acid hydrazides and by the reactions of aminoiminopyrimidines (prepared based on the above-mentioned carbonitriles) with acid chlorides.
- Vorob'ev,Kurbatov,Krasnikov,Mezheritskii,Usova
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p. 1492 - 1497
(2007/10/03)
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