SAR studies of 2-arylthiazolidine-4-carboxylic acid amides

A novel class of cytotoxic agents for prostate cancer

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

Research output: Contribution to journalArticle

15 Citations (Scopus)

Abstract

In our continuing efforts to develop novel chemotherapeutic agents for prostate cancer, recently we reported the discovery of 2-arylthiazolidine-4- carboxylic acid amides (ATCAAs) as a new class of cytotoxic agents. Several of them were very effective in killing specific human prostate cancer cell lines with low/sub-micromolar cytotoxicity and high selectivity against control cells in our sulforhodamine B assay. Encouraged with these preliminary results, we decided to further optimize this new scaffold to enhance the potency and selectivity. Current work describes the synthesis, SAR, and biological evaluation of new compounds for their ability to inhibit the growth of five human prostate cancer cell lines. The cytotoxicity data demonstrated that ATCAAs are sensitive to simple modifications or changes, which allowed us to understand the minimum structural requirements of this class of compounds to exhibit potent and selective anticancer activity against prostate cancer cells.

Original languageEnglish (US)
Pages (from-to)4010-4013
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume15
Issue number18
DOIs
StatePublished - Sep 15 2005

Fingerprint

Cytotoxins
Carboxylic Acids
Amides
Prostatic Neoplasms
Cells
Cytotoxicity
lissamine rhodamine B
Scaffolds
Cell Line
Assays
Growth

All Science Journal Classification (ASJC) codes

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

Cite this

SAR studies of 2-arylthiazolidine-4-carboxylic acid amides : A novel class of cytotoxic agents for prostate cancer. / Gududuru, Veeresa; Hurh, Eunju; Sullivan, Joshua; Dalton, James T.; Miller, Duane.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 15, No. 18, 15.09.2005, p. 4010-4013.

Research output: Contribution to journalArticle

Gududuru, Veeresa ; Hurh, Eunju ; Sullivan, Joshua ; Dalton, James T. ; Miller, Duane. / SAR studies of 2-arylthiazolidine-4-carboxylic acid amides : A novel class of cytotoxic agents for prostate cancer. In: Bioorganic and Medicinal Chemistry Letters. 2005 ; Vol. 15, No. 18. pp. 4010-4013.
@article{976f4805f2044acbbda069a577b04cdf,
title = "SAR studies of 2-arylthiazolidine-4-carboxylic acid amides: A novel class of cytotoxic agents for prostate cancer",
abstract = "In our continuing efforts to develop novel chemotherapeutic agents for prostate cancer, recently we reported the discovery of 2-arylthiazolidine-4- carboxylic acid amides (ATCAAs) as a new class of cytotoxic agents. Several of them were very effective in killing specific human prostate cancer cell lines with low/sub-micromolar cytotoxicity and high selectivity against control cells in our sulforhodamine B assay. Encouraged with these preliminary results, we decided to further optimize this new scaffold to enhance the potency and selectivity. Current work describes the synthesis, SAR, and biological evaluation of new compounds for their ability to inhibit the growth of five human prostate cancer cell lines. The cytotoxicity data demonstrated that ATCAAs are sensitive to simple modifications or changes, which allowed us to understand the minimum structural requirements of this class of compounds to exhibit potent and selective anticancer activity against prostate cancer cells.",
author = "Veeresa Gududuru and Eunju Hurh and Joshua Sullivan and Dalton, {James T.} and Duane Miller",
year = "2005",
month = "9",
day = "15",
doi = "10.1016/j.bmcl.2005.06.032",
language = "English (US)",
volume = "15",
pages = "4010--4013",
journal = "Bioorganic and Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Elsevier Limited",
number = "18",

}

TY - JOUR

T1 - SAR studies of 2-arylthiazolidine-4-carboxylic acid amides

T2 - A novel class of cytotoxic agents for prostate cancer

AU - Gududuru, Veeresa

AU - Hurh, Eunju

AU - Sullivan, Joshua

AU - Dalton, James T.

AU - Miller, Duane

PY - 2005/9/15

Y1 - 2005/9/15

N2 - In our continuing efforts to develop novel chemotherapeutic agents for prostate cancer, recently we reported the discovery of 2-arylthiazolidine-4- carboxylic acid amides (ATCAAs) as a new class of cytotoxic agents. Several of them were very effective in killing specific human prostate cancer cell lines with low/sub-micromolar cytotoxicity and high selectivity against control cells in our sulforhodamine B assay. Encouraged with these preliminary results, we decided to further optimize this new scaffold to enhance the potency and selectivity. Current work describes the synthesis, SAR, and biological evaluation of new compounds for their ability to inhibit the growth of five human prostate cancer cell lines. The cytotoxicity data demonstrated that ATCAAs are sensitive to simple modifications or changes, which allowed us to understand the minimum structural requirements of this class of compounds to exhibit potent and selective anticancer activity against prostate cancer cells.

AB - In our continuing efforts to develop novel chemotherapeutic agents for prostate cancer, recently we reported the discovery of 2-arylthiazolidine-4- carboxylic acid amides (ATCAAs) as a new class of cytotoxic agents. Several of them were very effective in killing specific human prostate cancer cell lines with low/sub-micromolar cytotoxicity and high selectivity against control cells in our sulforhodamine B assay. Encouraged with these preliminary results, we decided to further optimize this new scaffold to enhance the potency and selectivity. Current work describes the synthesis, SAR, and biological evaluation of new compounds for their ability to inhibit the growth of five human prostate cancer cell lines. The cytotoxicity data demonstrated that ATCAAs are sensitive to simple modifications or changes, which allowed us to understand the minimum structural requirements of this class of compounds to exhibit potent and selective anticancer activity against prostate cancer cells.

UR - http://www.scopus.com/inward/record.url?scp=23644435761&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=23644435761&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2005.06.032

DO - 10.1016/j.bmcl.2005.06.032

M3 - Article

VL - 15

SP - 4010

EP - 4013

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

SN - 0960-894X

IS - 18

ER -