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Synthesis, anticancer activity and mechanism of action of new phthalimido-1,3-thiazole derivatives. | LitMetric

AI Article Synopsis

  • A total of 22 new compounds were created and tested for their ability to kill cancer cells and peripheral blood mononuclear cells (PBMC).
  • The tests showed that all compounds were not cytotoxic to PBMCs at concentrations below 100 μM, but certain phthalimido-bis-1,3-thiazole compounds (5a-f) were particularly effective against tumor cells, reducing their viability to below 59%.
  • Based on their effectiveness, compounds 5b and 5e were chosen for further testing, highlighting the crucial role of the 1,3-thiazole structure in enhancing anti-tumor activity.

Article Abstract

In this work, 22 new compounds were obtained and evaluated for their cytotoxic activity on peripheral blood mononuclear cells (PBMC) and eight different tumor cell lines. All compounds displayed IC values above 100 μM when assayed against PBMCs. The cytotoxic assays in tumor cell lines revealed that sub-series of phthalimido-bis-1,3-thiazoles (5a-f) exhibited the best anti-tumor activity profile, presenting viability values below 59 %. As a result, the IC value was calculated for compounds 5a-f and 4c, and compounds 5b and 5e were selected for further assays due to their best ICs. Considering the results presented by the sub-series 5a-f, the importance of the 1,3-thiazole ring in improving the anti-tumor activity was pointed out. Together, the results highlighted the anti-tumor activity of phthalimido-bis-1,3-thiazole derivatives.

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Source
http://dx.doi.org/10.1016/j.cbi.2021.109597DOI Listing

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