About: Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: A template-based approach-Part 2.     Goto   Sponge   NotDistinct   Permalink

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  • Previous efforts by our group have established pyrazolo[1,5-a]pyrimidine as a viable core for the development of potent and selective CDK inhibitors. As part of an effort to utilize the pyrazolo[1,5-a]pyrimidine core as a template for the design and synthesis of potent and selective kinase inhibitors, we focused on a key regulator in the cell cycle progression, CHK1. Continued SAR development of the pyrazolo [1,5-a]pyrimidine core at the C5 and C6 positions, in conjunction with previously disclosed SAR at the C3 and C7 positions, led to the discovery of potent and selective CHK1 inhibitors.
  • Previous efforts by our group have established pyrazolo[1,5-a]pyrimidine as a viable core for the development of potent and selective CDK inhibitors. As part of an effort to utilize the pyrazolo[1,5-a]pyrimidine core as a template for the design and synthesis of potent and selective kinase inhibitors, we focused on a key regulator in the cell cycle progression, CHK1. Continued SAR development of the pyrazolo [1,5-a]pyrimidine core at the C5 and C6 positions, in conjunction with previously disclosed SAR at the C3 and C7 positions, led to the discovery of potent and selective CHK1 inhibitors. (en)
Title
  • Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: A template-based approach-Part 2.
  • Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: A template-based approach-Part 2. (en)
skos:prefLabel
  • Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: A template-based approach-Part 2.
  • Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: A template-based approach-Part 2. (en)
skos:notation
  • RIV/00216224:14310/11:00055928!RIV12-MSM-14310___
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • N
http://linked.open...iv/cisloPeriodika
  • 1
http://linked.open...vai/riv/dodaniDat
http://linked.open...aciTvurceVysledku
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http://linked.open...iv/duvernostUdaju
http://linked.open...titaPredkladatele
http://linked.open...dnocenehoVysledku
  • 194792
http://linked.open...ai/riv/idVysledku
  • RIV/00216224:14310/11:00055928
http://linked.open...riv/jazykVysledku
http://linked.open.../riv/klicovaSlova
  • Kinase CHK1 Pyrazolo[1 5-a]pyrimidine Template (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...odStatuVydavatele
  • US - Spojené státy americké
http://linked.open...ontrolniKodProRIV
  • [2CBB67421775]
http://linked.open...i/riv/nazevZdroje
  • Bioorganic & Medicinal Chemistry Letters
http://linked.open...in/vavai/riv/obor
http://linked.open...ichTvurcuVysledku
http://linked.open...cetTvurcuVysledku
http://linked.open...UplatneniVysledku
http://linked.open...v/svazekPeriodika
  • 21
http://linked.open...iv/tvurceVysledku
  • Alvarez, Carmen
  • Davis, Nicole
  • Duca, Jose
  • Dwyer, Michael
  • Fischmann, Thierry
  • Guzi, Timothy
  • Keertikar, Kerry
  • Labroli, Marc
  • Madison, Vincent
  • Parry, David
  • Paruch, Kamil
  • Poker, Cory
  • Rossman, Randall
  • Seghezzi, Wolfgang
  • Wiswell, Derek
issn
  • 0960-894X
number of pages
http://bibframe.org/vocab/doi
  • 10.1016/j.bmcl.2010.10.113
http://localhost/t...ganizacniJednotka
  • 14310
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