Ribociclib and palbociclib, two typical selective CDK4/6 inhibitors, which have been employed in clinic for the treatment of estrogen receptor positive (ER+) breast cancer, possess an active fragment of pyrrolo[2,3-d]pyrimidine and pyrido[2,3-d]pyrimidine, respectively. Herein, 25 novel pyrrolo(pyrido)[2,3-d]pyrimidine derivatives have been designed and synthesized based on molecular diversity. Their antiproliferative activity was evaluated against ER+ (T47D) and triple-negative (MDA-MB-436) breast cancer cell lines. The obtained results demonstrated that dihydroartemisinin-pyrrolo[2,3-d]pyrimidine and dihydroartemisinin-pyrido[2,3-d]pyrimidine derivatives are characterized by significant antiproliferative effects on both cell lines and have higher anticancer activity against triple-negative breast cancer cells compared to ribociclib.
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This research was supported by Guizhou Provincial Natural Science Foundation ([2019]1121) and Guizhou University Cultivation Project (No. [2020]83)
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Published in Khimiya Geterotsiklicheskikh Soedinenii, 2022, 58(8/9), 438–448
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Ding, J., Liu, T., Zeng, C. et al. Design, synthesis, and anti-breast-cancer activity evaluation of pyrrolo(pyrido)[2,3-d]pyrimidine derivatives. Chem Heterocycl Comp 58, 438–448 (2022). https://doi.org/10.1007/s10593-022-03110-w
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DOI: https://doi.org/10.1007/s10593-022-03110-w