4.7 Article

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

Journal

CHEMICO-BIOLOGICAL INTERACTIONS
Volume 347, Issue -, Pages -

Publisher

ELSEVIER IRELAND LTD
DOI: 10.1016/j.cbi.2021.109597

Keywords

Cancer; Anti-tumor activity; Phthalimide; Malignant melanoma; 1; 3-thiazole

Funding

  1. Conselho Nacional de Desenvolvimento Cientifico e Tecnologico (CNPq)
  2. Fundacao de Amparo a Ciencia e Tecnologia de Pernambuco (FACEPE)
  3. CNPq
  4. FACEPE [APQ-0350-4.03/18]

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The study identified that the phthalimidobis-1,3-thiazoles sub-series compounds exhibited good anti-tumor activity in tumor cell lines, with viability values below 59%. The importance of the 1,3-thiazole ring in enhancing anti-tumor activity was highlighted.
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 IC50 values above 100 mu M when assayed against PBMCs. The cytotoxic assays in tumor cell lines revealed that sub-series of phthalimidobis-1,3-thiazoles (5a-f) exhibited the best anti-tumor activity profile, presenting viability values below 59 %. As a result, the IC50 value was calculated for compounds 5a-f and 4c, and compounds 5b and 5e were selected for further assays due to their best IC50s. 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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