2. Academic Validation
  3. Benzoylphenylurea sulfur analogues with potent antitumor activity

Benzoylphenylurea sulfur analogues with potent antitumor activity

  • J Med Chem. 2006 Apr 6;49(7):2357-60. doi: 10.1021/jm051261s.
Gurulingappa Hallur 1,  Antonio Jimeno,  Susan Dalrymple,  Tao Zhu,  M Katherine Jung,  Manuel Hidalgo,  John T Isaacs,  Saraswati Sukumar,  Ernest Hamel,  Saeed R Khan
Affiliations

Affiliation

  • 1 Division of Chemical Therapeutics, The Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins, Baltimore, Maryland 21231, USA.
PMID: 16570932 DOI: 10.1021/jm051261s
Abstract

A novel series of BPU analogues were synthesized and evaluated for antitumor activity. In particular, BPU sulfur analogues 6n and 7d were shown to possess up to 10-fold increased potency, when compared to 1 (NSC-639829), against Cancer cell lines. 6n was more effective than 1 in causing Apoptosis of MCF-7 cells. When compared to other drugs with a similar mechanism of action, 6n retained significant ability to inhibit tubulin assembly, with an IC(50) of 2.1 microM.

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