2. Academic Validation
  3. Type 1 Phototherapeutic Agents. 2. Cancer Cell Viability and ESR Studies of Tricyclic Diarylamines

Type 1 Phototherapeutic Agents. 2. Cancer Cell Viability and ESR Studies of Tricyclic Diarylamines

  • ACS Med Chem Lett. 2012 Feb 16;3(4):284-8. doi: 10.1021/ml200266v.
Raghavan Rajagopalan 1,  Tien-Sung Lin 2,  Amolkumar S Karwa 1,  Amruta R Poreddy 1,  Bethel Asmelash 1,  Richard B Dorshow 1
Affiliations

Affiliations

  • 1 Covidien Pharmaceuticals , 675 McDonnell Boulevard, Hazelwood, Missouri 63042, United States.
  • 2 Department of Chemistry, Washington University , 1 Brookings Drive, St. Louis, Missouri 63130, United States.
PMID: 24900465 DOI: 10.1021/ml200266v
Abstract

Type 1 phototherapeutic agents based on diarylamines were assessed for free radical generation and evaluated in vitro for cell death efficacy in the U937 leukemia Cancer cell line. All of the compounds were found to produce copious free radicals upon photoexcitation with UV-A and/or UV-B light, as determined by electron spin resonance (ESR) spectroscopy. Among the diarylamines, the most potent compounds were acridan (4) and 9-phenylacridan (5), with IC50 values of 0.68 μM and 0.17 μM, respectively.

Keywords

Diarylamines; ESR; ROS; photosensitizers; radicals; type 1; type 2.

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