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- Title
Design, synthesis, and anti-breast-cancer activity evaluation of pyrrolo(pyrido)[2,3-d]pyrimidine derivatives.
- Authors
Ding, Jie; Liu, Tao; Zeng, Changguang; Li, Bingqing; Ai, Yi; Zhang, Xiaohan; Zhong, Hang
- Abstract
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.
- Subjects
PYRIMIDINES; PYRIMIDINE derivatives; TRIPLE-negative breast cancer; CYCLIN-dependent kinase inhibitors; ESTROGEN receptors; CELL lines
- Publication
Chemistry of Heterocyclic Compounds, 2022, Vol 58, Issue 8/9, p438
- ISSN
0009-3122
- Publication type
Article
- DOI
10.1007/s10593-022-03110-w