Synthesis and antiproliferative activity of 2-aryl-4-oxo-thiazolidin-3-yl- amides for prostate cancer

Veeresa Gududuru, Eunju Hurh, James T. Dalton, Duane Miller

Research output: Contribution to journalArticle

128 Citations (Scopus)

Abstract

We have previously described serine amide phosphates (SAPs) as a novel class of cytotoxic agents for prostate cancer. Several of them showed potent cytotoxicity against human prostate cancer cell lines, but were not selective in non-tumor cells. To improve the selectivity and further enhance the potency, we designed a new series of 2-aryl-4-oxo-thiazolidin-3-yl amides. The current work describes synthesis, SAR, and biological evaluation of these compounds for their ability to inhibit the growth of prostate cancer cells. The antiproliferative effects of synthesized compounds were examined in five human prostate cancer cell lines (DU-145, PC-3, LNCaP, PPC-1, and TSU), and in RH7777 cells (negative controls). From this study, three potent compounds (8, 20, and 21) have been detected, which are effective in killing prostate cancer cells with improved selectivity compared to SAPs.

Original languageEnglish (US)
Pages (from-to)5289-5293
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume14
Issue number21
DOIs
StatePublished - Nov 1 2004

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Amides
Prostatic Neoplasms
Cells
Phosphoserine
Serine
Phosphates
Cell Line
Cytotoxins
Cytotoxicity
Growth

All Science Journal Classification (ASJC) codes

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

Cite this

Synthesis and antiproliferative activity of 2-aryl-4-oxo-thiazolidin-3-yl- amides for prostate cancer. / Gududuru, Veeresa; Hurh, Eunju; Dalton, James T.; Miller, Duane.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 14, No. 21, 01.11.2004, p. 5289-5293.

Research output: Contribution to journalArticle

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