Benzoylphenylurea sulfur analogues with potent antitumor activity

Gurulingappa Hallur, Antonio Jimeno, Susan Dalrymple, Tao Zhu, M. Katherine Jung, Manuel Hidalgo, John Tod Isaacs, Saraswati Sukumar, Ernest Hamel, Saeed R. Khan

Research output: Contribution to journalArticle

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 μM.

Original languageEnglish (US)
Pages (from-to)2357-2360
Number of pages4
JournalJournal of Medicinal Chemistry
Volume49
Issue number7
DOIs
StatePublished - Apr 6 2006

Fingerprint

N-4-((5-bromo-2-pyrimidoxy)-3-methylphenyl)-(2-dimethylamino)benzoylurea
MCF-7 Cells
Tubulin
Sulfur
Cells
Apoptosis
Cell Line
Pharmaceutical Preparations
Neoplasms

ASJC Scopus subject areas

  • Organic Chemistry

Cite this

Hallur, G., Jimeno, A., Dalrymple, S., Zhu, T., Jung, M. K., Hidalgo, M., ... Khan, S. R. (2006). Benzoylphenylurea sulfur analogues with potent antitumor activity. Journal of Medicinal Chemistry, 49(7), 2357-2360. https://doi.org/10.1021/jm051261s

Benzoylphenylurea sulfur analogues with potent antitumor activity. / Hallur, Gurulingappa; Jimeno, Antonio; Dalrymple, Susan; Zhu, Tao; Jung, M. Katherine; Hidalgo, Manuel; Isaacs, John Tod; Sukumar, Saraswati; Hamel, Ernest; Khan, Saeed R.

In: Journal of Medicinal Chemistry, Vol. 49, No. 7, 06.04.2006, p. 2357-2360.

Research output: Contribution to journalArticle

Hallur, G, Jimeno, A, Dalrymple, S, Zhu, T, Jung, MK, Hidalgo, M, Isaacs, JT, Sukumar, S, Hamel, E & Khan, SR 2006, 'Benzoylphenylurea sulfur analogues with potent antitumor activity', Journal of Medicinal Chemistry, vol. 49, no. 7, pp. 2357-2360. https://doi.org/10.1021/jm051261s
Hallur G, Jimeno A, Dalrymple S, Zhu T, Jung MK, Hidalgo M et al. Benzoylphenylurea sulfur analogues with potent antitumor activity. Journal of Medicinal Chemistry. 2006 Apr 6;49(7):2357-2360. https://doi.org/10.1021/jm051261s
Hallur, Gurulingappa ; Jimeno, Antonio ; Dalrymple, Susan ; Zhu, Tao ; Jung, M. Katherine ; Hidalgo, Manuel ; Isaacs, John Tod ; Sukumar, Saraswati ; Hamel, Ernest ; Khan, Saeed R. / Benzoylphenylurea sulfur analogues with potent antitumor activity. In: Journal of Medicinal Chemistry. 2006 ; Vol. 49, No. 7. pp. 2357-2360.
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