Literature DB >> 18672368

4-(1H-indazol-5-yl)-6-phenylpyrimidin-2(1H)-one analogs as potent CDC7 inhibitors.

Cynthia M Shafer1, Mika Lindvall, Cornelia Bellamacina, Thomas G Gesner, Asha Yabannavar, Weiping Jia, Song Lin, Annette Walter.   

Abstract

A series of 4-(4-hydroxyphenyl)-6-phenylpyrimidin-2(1H)-ones were identified by HTS as inhibitors of CDC7. Molecular modeling and medicinal chemistry techniques were employed to explore the SAR for this series with a focus on removing potential metabolic liabilities and improving cellular potency.

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Year:  2008        PMID： 18672368     DOI： 10.1016/j.bmcl.2008.07.061

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  6 in total

1.  3D Pharmacophore Model-Assisted Discovery of Novel CDC7 Inhibitors.

Authors:  Mika Lindvall; Christopher McBride; Maureen McKenna; Thomas G Gesner; Asha Yabannavar; Kent Wong; Song Lin; Annette Walter; Cynthia M Shafer
Journal:  ACS Med Chem Lett       Date:  2011-08-02       Impact factor: 4.345

2.  Azaindole-Based Inhibitors of Cdc7 Kinase: Impact of the Pre-DFG Residue, Val 195.

Authors:  Yunsong Tong; Kent D Stewart; Alan S Florjancic; John E Harlan; Philip J Merta; Magdalena Przytulinska; Nirupama Soni; Kerren K Swinger; Haizhong Zhu; Eric F Johnson; Alexander R Shoemaker; Thomas D Penning
Journal:  ACS Med Chem Lett       Date:  2013-01-15       Impact factor: 4.345

3.  CDC7 inhibition blocks pathological TDP-43 phosphorylation and neurodegeneration.

Authors:  Nicole F Liachko; Pamela J McMillan; Chris R Guthrie; Thomas D Bird; James B Leverenz; Brian C Kraemer
Journal:  Ann Neurol       Date:  2013-07-08       Impact factor: 10.422

4.  Flexibility of the P-loop of Pim-1 kinase: observation of a novel conformation induced by interaction with an inhibitor.

Authors:  Lorien J Parker; Hisami Watanabe; Keiko Tsuganezawa; Yuri Tomabechi; Noriko Handa; Mikako Shirouzu; Hitomi Yuki; Teruki Honma; Naoko Ogawa; Tetsuo Nagano; Shigeyuki Yokoyama; Akiko Tanaka
Journal:  Acta Crystallogr Sect F Struct Biol Cryst Commun       Date:  2012-07-31

5.  Drug design with Cdc7 kinase: a potential novel cancer therapy target.

Authors:  Masaaki Sawa; Hisao Masai
Journal:  Drug Des Devel Ther       Date:  2009-02-06       Impact factor: 4.162

6.  Crystal structure of pim1 kinase in complex with a pyrido[4,3-d]pyrimidine derivative suggests a unique binding mode.

Authors:  Sang Jae Lee; Byeong-Gu Han; Jea-Won Cho; Jang-Sik Choi; Jaekyoo Lee; Ho-Juhn Song; Jong Sung Koh; Byung Il Lee
Journal:  PLoS One       Date:  2013-07-31       Impact factor: 3.240
  6 in total

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