Literature DB >> 19541484

Identification of substituted pyrazolo[1,5-a]quinazolin-5(4H)-one as potent poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors.

Federica Orvieto1, Danila Branca, Claudia Giomini, Philip Jones, Uwe Koch, Jesus M Ontoria, Maria Cecilia Palumbi, Michael Rowley, Carlo Toniatti, Ester Muraglia.   

Abstract

A novel series of pyrazolo[1,5-a]quinazolin-5(4H)-one derivatives proved to be a potent class of PARP-1 inhibitors. An extensive SAR around the 3-position of pyrazole in the scaffold led to the discovery of amides derivatives as low nanomolar PARP-1 inhibitors.

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Year:  2009        PMID: 19541484     DOI: 10.1016/j.bmcl.2009.05.113

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


  6 in total

1.  Active site fingerprinting and pharmacophore screening strategies for the identification of dual inhibitors of protein kinase C (ΡΚCβ) and poly (ADP-ribose) polymerase-1 (PARP-1).

Authors:  Navriti Chadha; Om Silakari
Journal:  Mol Divers       Date:  2016-05-23       Impact factor: 2.943

2.  Chemical structure-guided design of dynapyrazoles, cell-permeable dynein inhibitors with a unique mode of action.

Authors:  Jonathan B Steinman; Cristina C Santarossa; Rand M Miller; Lola S Yu; Anna S Serpinskaya; Hideki Furukawa; Sachie Morimoto; Yuta Tanaka; Mitsuyoshi Nishitani; Moriteru Asano; Ruta Zalyte; Alison E Ondrus; Alex G Johnson; Fan Ye; Maxence V Nachury; Yoshiyuki Fukase; Kazuyoshi Aso; Michael A Foley; Vladimir I Gelfand; James K Chen; Andrew P Carter; Tarun M Kapoor
Journal:  Elife       Date:  2017-05-19       Impact factor: 8.140

3.  Regioselectivity in the multicomponent reaction of 5-aminopyrazoles, cyclic 1,3-diketones and dimethylformamide dimethylacetal under controlled microwave heating.

Authors:  Kamal Usef Sadek; Ramadan Ahmed Mekheimer; Tahany Mahmoud Mohamed; Moustafa Sherief Moustafa; Mohamed Hilmy Elnagdi
Journal:  Beilstein J Org Chem       Date:  2012-01-04       Impact factor: 2.883

Review 4.  Quinazolinone and quinazoline derivatives: recent structures with potent antimicrobial and cytotoxic activities.

Authors:  Elham Jafari; Marzieh Rahmani Khajouei; Farshid Hassanzadeh; Gholam Hossein Hakimelahi; Ghadam Ali Khodarahmi
Journal:  Res Pharm Sci       Date:  2016 Jan-Feb

5.  Structure-Based Pharmacophore Modeling, Virtual Screening, Molecular Docking and Biological Evaluation for Identification of Potential Poly (ADP-Ribose) Polymerase-1 (PARP-1) Inhibitors.

Authors:  Yunjiang Zhou; Shi Tang; Tingting Chen; Miao-Miao Niu
Journal:  Molecules       Date:  2019-11-22       Impact factor: 4.411

6.  Antibacterial, antifungal and cytotoxic evaluation of some new 2,3-disubstituted 4(3H)-quinazolinone derivatives.

Authors:  G A Khodarahmi; M Rahmani Khajouei; G H Hakimelahi; D Abedi; E Jafari; F Hassanzadeh
Journal:  Res Pharm Sci       Date:  2012-07
  6 in total

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