Literature DB >> 17869522

Synthesis, biological evaluation and molecular modelling of sulfonohydrazides as selective PI3K p110alpha inhibitors.

Jackie D Kendall1, Gordon W Rewcastle, Raphael Frederick, Claire Mawson, William A Denny, Elaine S Marshall, Bruce C Baguley, Claire Chaussade, Shaun P Jackson, Peter R Shepherd.   

Abstract

A series of 2-methyl-5-nitrobenzenesulfonohydrazides were prepared and evaluated as inhibitors of PI3K. An isoquinoline derivative shows good selectivity for the p110alpha isoform over p110beta and p110delta, and also demonstrates good in vitro activity in a cell proliferation assay. Molecular modelling provides a rationalisation for the observed SAR.

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Year:  2007        PMID： 17869522     DOI： 10.1016/j.bmc.2007.08.062

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  8 in total

1.  Consensus model for identification of novel PI3K inhibitors in large chemical library.

Authors:  Chin Yee Liew; Xiao Hua Ma; Chun Wei Yap
Journal:  J Comput Aided Mol Des       Date:  2010-02-11       Impact factor: 3.686

2.  Molecular dynamics and integrated pharmacophore-based identification of dual [Formula: see text] inhibitors.

Authors:  Maninder Kaur; Pankaj Kumar Singh; Manjinder Singh; Renu Bahadur; Om Silakari
Journal:  Mol Divers       Date:  2017-11-14       Impact factor: 2.943

3.  Docking studies on isoform-specific inhibition of phosphoinositide-3-kinases.

Authors:  Dima A Sabbah; Jonathan L Vennerstrom; Haizhen Zhong
Journal:  J Chem Inf Model       Date:  2010-10-25       Impact factor: 4.956

4.  Phosphatidylinositol 3-kinase inhibitor (PIK75) containing surface functionalized nanoemulsion for enhanced drug delivery, cytotoxicity and pro-apoptotic activity in ovarian cancer cells.

Authors:  Meghna Talekar; Srinivas Ganta; Amit Singh; Mansoor Amiji; Jackie Kendall; William A Denny; Sanjay Garg
Journal:  Pharm Res       Date:  2012-06-01       Impact factor: 4.200

5.  4-[(1,3-Dioxo-2,3-dihydro-1H-benzo[de]isoquinolin-2-yl)meth-yl]-N'-[(E)-4-nitro-benzyl-idene]benzene-sulfono-hydrazide dimethyl sulfoxide monosolvate.

Authors:  Adailton J Bortoluzzi; Everton B Policarpi; Cristiano Mora; Kely N Oliveira; Ricardo J Nunes
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-02-12

Review 6.  Progress in the preclinical discovery and clinical development of class I and dual class I/IV phosphoinositide 3-kinase (PI3K) inhibitors.

Authors:  S J Shuttleworth; F A Silva; A R L Cecil; C D Tomassi; T J Hill; F I Raynaud; P A Clarke; P Workman
Journal:  Curr Med Chem       Date:  2011       Impact factor: 4.530

7.  Novel Thiochromanone Derivatives Containing a Sulfonyl Hydrazone Moiety: Design, Synthesis, and Bioactivity Evaluation.

Authors:  Lu Yu; Jiyan Chi; Lingling Xiao; Jie Li; Zhangfei Tang; Shuming Tan; Pei Li
Journal:  Molecules       Date:  2021-05-14       Impact factor: 4.411

Review 8.  A review exploring biological activities of hydrazones.

Authors:  Garima Verma; Akranth Marella; Mohammad Shaquiquzzaman; Mymoona Akhtar; Mohammad Rahmat Ali; Mohammad Mumtaz Alam
Journal:  J Pharm Bioallied Sci       Date:  2014-04
  8 in total

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