Synthesis of novel arylaminoquinazolinylurea derivatives and their antiproliferative activities against bladder cancer cell line

Jung Hun Kim, Yeonui Kwak, Chiman Song, Eun Joo Roh, Chang Hyun Oh, So Ha Lee, Taebo Sim, Jung Hoon Choi, Kyung Ho Yoo

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1 Citation (Scopus)


A novel series of arylurea and arylamide derivatives 1a–z, 2a–d having aminoquinazoline scaffold was designed and synthesized. Their in vitro antiproliferative activities against RT112 bladder cancer cell line and inhibitory activities against FGFR3 kinase were tested. Most compounds showed good antiproliferative activities against RT112 bladder cancer cell line, and arylurea compounds 1a–z were more potent than arylamide compounds 2a–d. Among them, eight compounds 1a, 1d–g, 1l, 1y, and 1z showed potent activities with GI50 values below submicromolar range. Especially, arylurea compounds 1d and 1g possessing 2,3-dimethyl and 3,4-dimethyl moieties exhibited superior or similar antiproliferative activity (GI50 = 8.8 nM and 30.2 nM, respectively) to AZD4547 (GI50 = 29.2 nM) as a reference standard.

Original languageEnglish
Pages (from-to)5082-5086
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Issue number20
Publication statusPublished - 2016 Oct 15



  • Antiproliferative activity
  • Arylaminoquinazolinylamides
  • Arylaminoquinazolinylureas
  • Bladder cancer cell line
  • Enzymatic activity
  • FGFR3

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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