Anticancer Polymers via the Biginelli Reaction
Posted on 2020-08-18 - 11:37
We
developed a polymer–drug strategy to explore anticancer polymers.
A series of monomers containing groups with potential anticancer activity
have been facilely prepared through the Biginelli reaction. These
monomers were used to produce water-soluble polymers through convenient
radical copolymerization. The resulting polymers are biocompatible
and can be directly used to suppress proliferation of different cancer
cells without the release of small molecules. Theoretical calculations
revealed that Biginelli groups in polymers had strong interaction
with the Eg5 protein, which is highly expressed in cancer cells and
is closely related to cell mitosis. Subsequent cell experiments confirmed
that a screened polymer is efficient in inhibiting mitosis in different
cancer cells. Our study of exploring functional polymers via the combination
of multicomponent reactions and theoretical calculation resulted in
promising anticancer polymers, which might pave a path for de novo
designing of functional polymers and have important implications in
the fields of organic, computational, and polymer chemistry.
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Li, Yongsan; Tan, Tianhao; Zhao, Yuan; Wei, Yen; Wang, Dong; Chen, Rongjun; et al. (2020). Anticancer Polymers via the Biginelli Reaction. ACS Publications. Collection. https://doi.org/10.1021/acsmacrolett.0c00496
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AUTHORS (7)
YL
Yongsan Li
TT
Tianhao Tan
YZ
Yuan Zhao
YW
Yen Wei
DW
Dong Wang
RC
Rongjun Chen
LT
Lei Tao