Literature DB >> 23987476

Phenylpyrazolo[1,5-a]quinazolin-5(4H)-one: a suitable scaffold for the development of noncamptothecin topoisomerase I (Top1) inhibitors.

Sabrina Taliani1, Isabella Pugliesi, Elisabetta Barresi, Silvia Salerno, Christophe Marchand, Keli Agama, Francesca Simorini, Concettina La Motta, Anna Maria Marini, Francesco Saverio Di Leva, Luciana Marinelli, Sandro Cosconati, Ettore Novellino, Yves Pommier, Roberto Di Santo, Federico Da Settimo.   

Abstract

In search for a novel chemotype to develop topoisomerase I (Top1) inhibitors, the pyrazolo[1,5-a]quinazoline nucleus, structurally related to the indenoisoquinoline system precursor of well-known Top1 poisons, was variously decorated (i.e., a substituted phenyl ring at 2- or 3-position, a protonable side chain at 4- or 5-position), affording a number of Top1 inhibitors with cleavage patterns common to CPT and MJ-III-65. SARs data were rationalized by means of an advanced docking protocol.

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Year:  2013        PMID： 23987476      PMCID： PMC3982121          DOI： 10.1021/jm400932c

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  16 in total

1.  The mechanism of topoisomerase I poisoning by a camptothecin analog.

Authors:  Bart L Staker; Kathryn Hjerrild; Michael D Feese; Craig A Behnke; Alex B Burgin; Lance Stewart
Journal:  Proc Natl Acad Sci U S A       Date:  2002-11-08       Impact factor: 11.205

2.  Cellular topoisomerase I inhibition and antiproliferative activity by MJ-III-65 (NSC 706744), an indenoisoquinoline topoisomerase I poison.

Authors:  Smitha Antony; Glenda Kohlhagen; Keli Agama; Muthusamy Jayaraman; Shousong Cao; Farukh A Durrani; Youcef M Rustum; Mark Cushman; Yves Pommier
Journal:  Mol Pharmacol       Date:  2004-11-05       Impact factor: 4.436

Review 3.  Repair of topoisomerase I-mediated DNA damage.

Authors:  Yves Pommier; Juana M Barcelo; V Ashutosh Rao; Olivier Sordet; Andrew G Jobson; Laurent Thibaut; Ze-Hong Miao; Jennifer A Seiler; Hongliang Zhang; Christophe Marchand; Keli Agama; John L Nitiss; Christophe Redon
Journal:  Prog Nucleic Acid Res Mol Biol       Date:  2006

Review 4.  Topoisomerase I inhibitors: camptothecins and beyond.

Authors:  Yves Pommier
Journal:  Nat Rev Cancer       Date:  2006-10       Impact factor: 60.716

Review 5.  Current perspectives on the clinical experience, pharmacology, and continued development of the camptothecins.

Authors:  Rocio Garcia-Carbonero; Jeffrey G Supko
Journal:  Clin Cancer Res       Date:  2002-03       Impact factor: 12.531

Review 6.  Drugging topoisomerases: lessons and challenges.

Authors:  Yves Pommier
Journal:  ACS Chem Biol       Date:  2013-01-04       Impact factor: 5.100

7.  Dialkylaminoalkylindolonaphthyridines as potential antitumour agents: synthesis, cytotoxicity and DNA binding properties.

Authors:  Lisa Dalla Via; Ornella Gia; Sebastiano Marciani Magno; Antonio Da Settimo; Giampaolo Primofiore; Federico Da Settimo; Francesca Simorini; Anna Maria Marini
Journal:  Eur J Med Chem       Date:  2002-06       Impact factor: 6.514

8.  One-pot microwave assisted preparation of pyrazoloquinazolinone libraries.

Authors:  Thomas E Vasquez; Thomas Nixey; Balan Chenera; Vijay Gore; Michael D Bartberger; Yaxiong Sun; Christopher Hulme
Journal:  Mol Divers       Date:  2003       Impact factor: 2.943

9.  The structural basis of camptothecin interactions with human serum albumin: impact on drug stability.

Authors:  T G Burke; Z Mi
Journal:  J Med Chem       Date:  1994-01-07       Impact factor: 7.446

10.  Differential induction of topoisomerase I-DNA cleavage complexes by the indenoisoquinoline MJ-III-65 (NSC 706744) and camptothecin: base sequence analysis and activity against camptothecin-resistant topoisomerases I.

Authors:  Smitha Antony; Muthusamy Jayaraman; Gary Laco; Glenda Kohlhagen; Kurt W Kohn; Mark Cushman; Yves Pommier
Journal:  Cancer Res       Date:  2003-11-01       Impact factor: 12.701
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  5 in total

1.  Discovery of potent indenoisoquinoline topoisomerase I poisons lacking the 3-nitro toxicophore.

Authors:  Daniel E Beck; Monica Abdelmalak; Wei Lv; P V Narasimha Reddy; Gabrielle S Tender; Elizaveta O'Neill; Keli Agama; Christophe Marchand; Yves Pommier; Mark Cushman
Journal:  J Med Chem       Date:  2015-04-24       Impact factor: 7.446

2.  Discovery of Pyrido[3',2':5,6]thiopyrano[4,3-d]pyrimidine-Based Antiproliferative Multikinase Inhibitors.

Authors:  Silvia Salerno; Elisabetta Barresi; Aída Nelly García-Argáez; Sabrina Taliani; Francesca Simorini; Giorgio Amendola; Stefano Tomassi; Sandro Cosconati; Ettore Novellino; Federico Da Settimo; Anna Maria Marini; Lisa Dalla Via
Journal:  ACS Med Chem Lett       Date:  2019-01-17       Impact factor: 4.345

Review 3.  An insight into the therapeutic potential of quinazoline derivatives as anticancer agents.

Authors:  Irshad Ahmad
Journal:  Medchemcomm       Date:  2017-04-07       Impact factor: 3.597

4.  Temporal and Wash-Out Studies Identify Medicines for Malaria Venture Pathogen Box Compounds with Fast-Acting Activity against Both Trypanosoma cruzi and Trypanosoma brucei.

Authors:  Melissa L Sykes; Emily K Kennedy; Kevin D Read; Marcel Kaiser; Vicky M Avery
Journal:  Microorganisms       Date:  2022-06-25

5.  Synthesis and cytotoxic evaluation of novel quinazolinone derivatives as potential anticancer agents.

Authors:  Safoora Poorirani; Sedighe Sadeghian-Rizi; Ghadamali Khodarahmi; Marzieh Rahmani Khajouei; Farshid Hassanzadeh
Journal:  Res Pharm Sci       Date:  2018-10
  5 in total

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