Wang, Xuebao published the artcileDiscovery of N-substituted sulfamoylbenzamide derivatives as novel inhibitors of STAT3 signaling pathway based on Niclosamide, Safety of (2-Methoxyphenyl)methanamine, the publication is European Journal of Medicinal Chemistry (2021), 113362, database is CAplus and MEDLINE.
Signal transducer and activator of transcription 3 (STAT3) has been confirmed as an attractive therapeutic target for cancer therapy. Herein, a series of N-substituted sulfamoylbenzamide STAT3 inhibitors I [R1 = H, OH; R2 = H, Cl; R3 = 2-MeOC6H4, 3,4,5-(OMe)3C6H2, 3-MeOC6H4CH2, etc.; R4 = H, C(O)Me, C(O)Ph, etc.] based on small-mol. STAT3 inhibitor Niclosamide was synthesized. Compound I [R1 = H, R2 = Cl, R3 = 4-CO2t-BuC6H4, R4 = H] the best active compound of this series, was identified as an inhibitor of IL-6/STAT3 signaling with an IC50 of 0.61-1.11μM in MDA-MB-231, HCT-116 and SW480 tumor cell lines with STAT3 overexpression, by inhibiting the phosphorylation of STAT3 of Tyr705 residue and the expression of STAT3 downstream genes, inducing apoptosis and inhibiting the migration of cancer cells. Furthermore, in vivo study revealed that compound I [R1 = H, R2 = Cl, R3 = 4-CO2t-BuC6H4, R4 = H] suppressed the MDA-MB-231 xenograft tumor growth in nude mice at the dose of 30 mg/kg (i.g.), which has better antitumor activity than the pos. control Niclosamide. More importantly, compound I [R1 = H, R2 = Cl, R3 = 4-CO2t-BuC6H4, R4 = H] was an orally bioavailable anticancer agent as a promising candidate for further development.
European Journal of Medicinal Chemistry published new progress about 6850-57-3. 6850-57-3 belongs to ethers-buliding-blocks, auxiliary class Amine,Benzene,Ether, name is (2-Methoxyphenyl)methanamine, and the molecular formula is C10H10O2, Safety of (2-Methoxyphenyl)methanamine.
Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem