Literature DB >> 12657262

Novel indole-based inhibitors of IMPDH: introduction of hydrogen bond acceptors at indole C-3.

Scott H Watterson1, T G Murali Dhar, Shelley K Ballentine, Zhongqi Shen, Joel C Barrish, Daniel Cheney, Catherine A Fleener, Katherine A Rouleau, Robert Townsend, Diane L Hollenbaugh, Edwin J Iwanowicz.   

Abstract

The development of a series of novel indole-based inhibitors of 5'-inosine monophosphate dehydrogenase (IMPDH) is described. Various hydrogen bond acceptors at C-3 of the indole were explored. The synthesis and the structure-activity relationships (SARs) derived from in vitro studies are outlined.

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Year:  2003        PMID: 12657262     DOI: 10.1016/s0960-894x(03)00109-4

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


  7 in total

Review 1.  IMP dehydrogenase: structure, mechanism, and inhibition.

Authors:  Lizbeth Hedstrom
Journal:  Chem Rev       Date:  2009-07       Impact factor: 60.622

Review 2.  Inhibitors of inosine 5'-monophosphate dehydrogenase as emerging new generation antimicrobial agents.

Authors:  Kapil Juvale; Althaf Shaik; Sivapriya Kirubakaran
Journal:  Medchemcomm       Date:  2019-05-02       Impact factor: 3.597

Review 3.  Recent advances in the pharmacological diversification of quinazoline/quinazolinone hybrids.

Authors:  Prashant S Auti; Ginson George; Atish T Paul
Journal:  RSC Adv       Date:  2020-11-12       Impact factor: 4.036

4.  In silico design of human IMPDH inhibitors using pharmacophore mapping and molecular docking approaches.

Authors:  Rui-Juan Li; Ya-Li Wang; Qing-He Wang; Jian Wang; Mao-Sheng Cheng
Journal:  Comput Math Methods Med       Date:  2015-02-15       Impact factor: 2.238

5.  Synthesis, Biological Evaluation and Molecular Docking of Novel Indole-Aminoquinazoline Hybrids for Anticancer Properties.

Authors:  Malose J Mphahlele; Mmakwena M Mmonwa; Abimbola Aro; Lyndy J McGaw; Yee Siew Choong
Journal:  Int J Mol Sci       Date:  2018-07-31       Impact factor: 5.923

6.  Synthesis and Evaluation of N-(3-Trifluoroacetyl-indol-7-yl) Acetamides for Potential In Vitro Antiplasmodial Properties.

Authors:  Malose J Mphahlele; Mmakwena M Mmonwa; Yee Siew Choong
Journal:  Molecules       Date:  2017-07-02       Impact factor: 4.411

7.  Synthesis, Evaluation of Cytotoxicity and Molecular Docking Studies of the 7-Acetamido Substituted 2-Aryl-5-bromo-3-trifluoroacetylindoles as Potential Inhibitors of Tubulin Polymerization.

Authors:  Malose J Mphahlele; Nishal Parbhoo
Journal:  Pharmaceuticals (Basel)       Date:  2018-06-11
  7 in total

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