Small Molecules
Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction
and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting
Antitumor Agents
Version 2 2018-08-09, 19:05
Version 1 2018-08-09, 19:03
Posted on 2018-08-09 - 19:05
p53-Murine double
minute 2 (MDM2) interaction and histone deacetylases (HDACs) are important
targets in antitumor drug development. Inspired by the synergistic
effects between MDM2 and HDACs, the first MDM2/HDACs dual inhibitors
were identified, which showed excellent activities against both targets.
In particular, compound 14d was proven to be a potent
and orally active MDM2/HDAC dual inhibitor, whose antitumor mechanisms
were validated in cancer cells. Compound 14d showed excellent
in vivo antitumor potency in the A549 xenograft model, providing a
promising lead compound for the development of novel antitumor agents.
Also, this proof-of-concept study offers a novel and efficient strategy
for multitargeting antitumor drug discovery.
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He, Shipeng; Dong, Guoqiang; Wu, Shanchao; Fang, Kun; Miao, Zhenyuan; Wang, Wei; et al. (2018). Small Molecules
Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction
and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting
Antitumor Agents. ACS Publications. Collection. https://doi.org/10.1021/acs.jmedchem.8b00664
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AUTHORS (7)
SH
Shipeng He
GD
Guoqiang Dong
SW
Shanchao Wu
KF
Kun Fang
ZM
Zhenyuan Miao
WW
Wei Wang
CS
Chunquan Sheng
KEYWORDS
antitumor drug developmentSmall Moleculescompound 14cancer cellsHDACantitumor mechanismsminute 2Inhibiting p 53-Murine Double Minute 2Compound 14multitargeting antitumor drug discoveryMDM 2proof-of-concept studyvivo antitumor potencyHistone DeacetylasesNovel Multitargeting Antitumor Agents p 53-Murine549 xenograft modelhistone deacetylasesnovel antitumor agentsinhibitor