SAR studies of 2-arylthiazolidine-4-carboxylic acid amides: a novel class of cytotoxic agents for prostate cancer.
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.
Gududuru
Veeresa
V
Department of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, TN 38163, USA.
Hurh
Eunju
E
Sullivan
Joshua
J
Dalton
James T
JT
Miller
Duane D
DD
D000577:Amides / Q000737:chemistry* / Q000494:pharmacology / Q000633:toxicity*; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000145:classification / Q000494:pharmacology / Q000633:toxicity*; D002264:Carboxylic Acids / Q000737:chemistry*; D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D008297:Male; D015394:Molecular Structure; D011471:Prostatic Neoplasms / Q000473:pathology*; D013329:Structure-Activity Relationship
D000577:Amides; D000970:Antineoplastic Agents; D002264:Carboxylic Acids