Pharmacophore identification of c-Myc inhibitor 10074-G5
Graphical abstract
Section snippets
Acknowledgments
Financial support for this work is gratefully acknowledged from the University of Maryland School of Pharmacy (SF), an American Chemical Society Pre-Doctoral Medicinal Chemistry Fellowship (JLY) and NIH grant R01 CA140624 (EVP).
References and notes (27)
- et al.
Mol. Cell.
(1999) - et al.
Exp. Hematol.
(2006) - et al.
Cell
(2003) - et al.
Cell
(1991) - et al.
Bioorg. Med. Chem.
(2006) - et al.
Chem. Biol.
(2006) - et al.
Bioorg. Med. Chem. Lett.
(2009) - et al.
Chem. Biol.
(2008) Mol. Cell. Biol.
(1999)- et al.
Oncogene
(1999)
Oncogene
Med. Chem. Commun.
Cited by (58)
MYC the oncogene from hell: Novel opportunities for cancer therapy
2024, European Journal of Medicinal ChemistrySynthesis and biological evaluation of a novel c-Myc inhibitor against colorectal cancer via blocking c-Myc/Max heterodimerization and disturbing its DNA binding
2022, European Journal of Medicinal ChemistryMYC oncogenes as potential anticancer targets
2022, Oncogenic Viruses: Volume 2: Medical Applications of Viral Oncology ResearchTargeting MYC: From understanding its biology to drug discovery
2021, European Journal of Medicinal ChemistryCitation Excerpt :Computational structure similarity searching for compounds in which the 6-membered ethylbenzylidene and five-membered rhodanine rings of 10058-F4 were varied has led to synthetic derivative #474, which exhibits a 10-fold improvement of potency [114]. Pharmacore analysis of 10074-G5 determined the nitro and oxadiazole moieties of the benzofuran derivative to be essential for inhibitory activity against MYC heterodimerization [115]. Analogue JY-3-094, in which the biphenyl group has been replaced by para-substituted benzoic acid, shows a 10-fold improvement in potency (as assessed by electrophoretic mobility shift assay (EMSA)) but poor cellular uptake in HL-60 cells.
Discovery of 4-(3,5-dimethoxy-4-(((4-methoxyphenethyl)amino)methyl)phenoxy)-N-phenylaniline as a novel c-myc inhibitor against colorectal cancer in vitro and in vivo
2020, European Journal of Medicinal ChemistryCitation Excerpt :Thus, c-Myc inhibitors could help to suppress the initiation and progression of tumors. Recently, lots of c-Myc inhibitors were discovered including Myc-Max protein-protein interactions [17–19], such as 10058-F4, 10074-G5, SF-4-017, NUCC-0176242, or Myc-Max protein-DNA binding interactions [20,21], such as Mycro 3, KJ Pyr 9, or binding to c-Myc G-quadruplex(G4) stabilizers [22,23], such as Indenoisoquinoline 5, IZCZ-3, etc. Despite plenty of c-Myc inhibitors (shown in Fig. 1) reported, there is no anti-Myc drug clinically available.
- †
These authors contributed equally to this work.