Synthesis, anticancer activity and mechanism of action of new phthalimido-1,3-thiazole derivatives.
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 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 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.
['Oliveira|Arsênio Rodrigues|AR|', 'Dos Santos|Flaviana Alves|FA|', 'Ferreira|Larissa Pelágia de Lima|LPL|', 'Pitta|Maira Galdino da Rocha|MGDR|', 'Silva|Marcius Vinicius de Oliveira|MVO|', 'Cardoso|Marcos Verissimo de Oliveira|MVO|', 'Pinto|Aline Ferreira|AF|', 'Marchand|Pascal|P|', 'de Melo Rêgo|Moacyr Jesus Barreto|MJB|', 'Leite|Ana Cristina Lima|ACL|']
D000970:Antineoplastic Agents D002460:Cell Line D045744:Cell Line, Tumor D049109:Cell Proliferation D004354:Drug Screening Assays, Antitumor D018922:HL-60 Cells D006801:Humans D020014:K562 Cells D007963:Leukocytes, Mononuclear D015394:Molecular Structure D013329:Structure-Activity Relationship D013844:Thiazoles
Anti-tumor activity 1,3-thiazole Cancer Malignant melanoma Phthalimide