83393-46-8Relevant academic research and scientific papers
Synthesis and evaluation of C3 substituted chalcone-based derivatives of 7-azaindole as protein kinase inhibitors
Qhobosheane, Malikotsi A.,Legoabe, Lesetja J.,Josselin, Béatrice,Bach, Stéphane,Ruchaud, Sandrine,Beteck, Richard M.
, p. 1395 - 1407 (2020)
Chalcones are a group of naturally occurring or synthetic compounds which possess a wide range of biological activities. In this paper, a series of twenty-three 7-azaindole-chalcone hybrids (5a–w) were synthesized and evaluated as potential protein kinase inhibitors. Analyses of structure–activity relationships revealed that some of these compounds exhibit significant activity against Haspin kinase, with compounds 5f and 5q exhibiting IC50 values of 0.47 and 0.41?μM, respectively. Furthermore, 5f also inhibits cyclin-dependent kinase 9 (CDK9/CyclinT) in a micromolar potency (IC50?=?2.26?μM). This novel dual-target inhibitor is a promising lead for the development of chemopreventive/chemotherapeutic agents.
Discovery of novel 4-azaaryl-N-phenylpyrimidin-2-amine derivatives as potent and selective FLT3 inhibitors for acute myeloid leukaemia with FLT3 mutations
Long, Yi,Yu, Mingfeng,Ochnik, Aleksandra M.,Karanjia, Jasmine D.,Basnet, Sunita KC.,Kebede, Alemwork A.,Kou, Lianmeng,Wang, Shudong
, (2021/02/03)
Feline McDonough sarcoma (FMS)-like tyrosine kinase 3 (FLT3) is one of the most pursued targets in the treatment of acute myeloid leukaemia (AML) as its gene amplification and mutations, particularly internal tandem duplication (ITD), contribute to the pa
Synthesis and antibacterial evaluation of (E)-1-(1H-indol-3-yl) ethanone O-benzyl oxime derivatives against MRSA and VRSA strains
Akunuri, Ravikumar,Veerareddy, Vaishnavi,Kaul, Grace,Akhir, Abdul,Unnissa, Tanveer,Parupalli, Ramulu,Madhavi,Chopra, Sidharth,Nanduri, Srinivas
, (2021/08/27)
Infections caused due to multidrug resistant organisms have emerged as a constant menace to human health. Even though numerous antibiotics are currently available for treating infectious diseases, a great number of bacterial strains have acquired resistance to many of them. Among these, infections caused due to Staphylococcus aureus are predominant in adult and paediatric population. Indole is a prominent chemical scaffold found in many pharmacologically active natural products and synthetic drugs. A number of oxime ether containing compounds have attracted attention of researchers owing to their interesting biological properties. Current work details the synthesis of indole containing oxime ether derivatives and their evaluation for antimicrobial activity against a panel of bacterial and mycobacterial strains. Synthesized compounds demonstrated good to moderate activity against drug-resistant S. aureus including resistant to vancomycin. Among all, compound 5h was found to possess potent activity against susceptible as well as MRSA and VRSA strains of S. aureus with MIC of 1 μg/mL and 2–4 μg/mL respectively. In addition, compound 5h was found to be non-toxic to Vero cells and exhibited good selectivity index of >40. Further, 5h, E-9a and E-9b possessed good biofilm inhibition against S. aureus. With these assuring biological properties, synthesized compounds could be potential prospective antimicrobial agents.
Amino dithio-formate compound and its preparation method and application
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Paragraph 0188; 0189, (2017/11/24)
The invention discloses novel aminodithioformate compounds, and a preparation method and application thereof, belonging to the field of pharmaceutical chemistry. The structure of the compounds is disclosed as formula I. The research proves that the compou
Double (amino-sulfur generation of formic acid ) - 1,3-propane diester compound and its synthetic method, pharmaceutical composition and use thereof
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Paragraph 0296-0299, (2016/10/08)
The invention relates to a bis(aminodithioformate)-1,3-propane diester compound, and synthesis method thereof, a pharmaceutical composition containing the compound and a use, and especially relates to the use in preparing drugs for treating or preventing cancers. The compound is represented as the formula (I), wherein A is selected from substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heterocyclic group, R1 and R2 are the same or different and are independently selected from hydrogen, alkyl, aryl alkyl or heteroaryl alkyl, or a substituted or unsubstituted heterocyclic ring formed together by the R1, the R2 and an N atom connected with the R1 and the R2.
4 (PYRROLOPYRIDINYL)PYRIMIDINYL-2-AMINE DERIVATIVES
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Page/Page column 11-12, (2010/07/10)
Compounds of the formula I in which R1, R2, R3, R4 and R5 are each as defined in claim 1 are inhibitors of cell proliferation/cell vitality and can be used to treat tumors.
Novel heterocycle-substituted pyrimidines as inhibitors of NF-κB transcription regulation related to TNF-α cytokine release
Ha, Hyung-Ho,Kim, Jee Seon,Kim, B. Moon
, p. 653 - 656 (2008/12/23)
Novel heterocyclic ring-substituted pyrimidines have been designed as inhibitors of glycogen synthase kinase-3β (GSK-3β) from the modification of known inhibitors. Several potent inhibitors exhibiting nanomolar activities were discovered against GSK-3β kinase as well as in an NF-κB reporter gene assay. Based on the results from in vitro TNF-α release inhibition and in vivo endotoxima, these inhibitors are expected to be useful candidates for treatment of inflammation-related diseases.
PYRIDINONYL PDK1 INHIBITORS
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Page/Page column 96, (2008/06/13)
The present invention provides pyridinonyl PDKl inhibitors and methods of treating cancer using the same.
Azaindolylidene derivatives as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
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Page/Page column 38, (2010/11/27)
The present invention is directed to compounds of the formula or pharmaceutically acceptable salts, prodrug, solvate or optical isomer thereof, pharmaceutical compositions containing same and use thereof for treating diseases linked to disregulated cell p
BICYCLIC NITROGEN COMPOUNDS AS MODULATORS OF GHRELIN RECEPTOR AND USES THEREOF
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Page/Page column 83, (2010/11/28)
Disclosed herein are compounds of Formula I as defined herein, or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof, that modulates the activity of a ghrelin receptor. Disclosed herein are also methods of treating diseases or conditions that comprise administering to a subject in need thereof a therapeutically effective amount of a compound of Formula I.
