Dual inhibitors of inosine monophosphate dehydrogenase and histone deacetylase based on a cinnamic hydroxamic acid core structure.

Bioorganic & Medicinal Chemistry
Liqiang ChenKrzysztof W Pankiewicz

Abstract

Small molecules that act on multiple biological targets have been proposed to combat the drug resistance commonly observed for cancer chemotherapy. By combining the structural features of known inhibitors of inosine monophosphate dehydrogense (IMPDH) and histone deacetylase (HDAC), dual inhibitors of IMPDH and HDAC based on the scaffold of cinnamic hydroxamic acid (CHA) have been designed, synthesized, and evaluated in biological assays. Key features, including the linker length, linker functionality, substitution position, and interacting groups, have been explored. Their individual contribution to the inhibitory activities against human IMPDH1 and IMPDH2 as well as HDAC has been assessed.

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Citations

Sep 4, 2013·European Journal of Medicinal Chemistry·Zhao-Jin ZhongZhuo-Rong Li
Sep 10, 2014·Journal of Enzyme Inhibition and Medicinal Chemistry·Grzegorz CholewińskiKrystyna Dzierzbicka
Dec 4, 2014·European Journal of Medicinal Chemistry·Reshma Rani, Carlotta Granchi
Feb 24, 2019·International Journal of Molecular Sciences·Chiara ZagniNicola Micale
Mar 29, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Regina MartínezBeatriz de Pascual-Teresa
Oct 20, 2018·Current Medicinal Chemistry·Loredana CappellacciRiccardo Petrelli
Feb 19, 2016·ChemMedChem·A Ganesan
May 8, 2018·Medicinal Research Reviews·Heba M HeshamKhaled A M Abouzid
Apr 30, 2020·ChemMedChem·Michael MorgenAubry K Miller
Nov 5, 2020·European Journal of Medicinal Chemistry·Gargi Nikhil VaidyaDinesh Kumar
Oct 21, 2020·European Journal of Medicinal Chemistry·Amr K A BassGamal El-Din A Abuo-Rahma
Aug 15, 2018·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·Akhilesh Kumar ShuklaJyoti Pandey

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