Yu, Ming-jun published the artcileStructure-activity relationship studies on Pd176252 derivatives leading to discovery of novel GRP receptor antagonist with potent anticancer activity, Recommanded Product: 4-Nitrophenylacetic acid, the publication is Medicinal Chemistry Research (2021), 30(11), 2069-2089, database is CAplus.
Abstract: Gastrin-releasing peptide (GRP)/gastrin-releasing peptide receptor (GRPR) have various physiol. effects, and many studies report that GRPR is a potential anticancer target. Pd176252 is a typical small-mol. GRPR antagonist that exhibits anti-proliferation activity against most cancers. In this study, 31 novel Pd176252 analogs were designed, synthesized, and evaluated for anti-proliferation activity against human prostate cancer (PC3), mouse pancreatic cancer (Pan02), human gastric cancer (HGC-27), and hepatocellular carcinoma (HepG2) cell lines. Of all the compounds evaluated, 5a and 6e showed better anti-proliferation activity compared to Pd176252 against PC3 (half-maximal inhibitory concentration [IC50] = 4.97 and 9.88 ¦ÌM, resp.), Pan02 (IC50 = 4.36 and 2.50 ¦ÌM, resp.), and HGC-27 (IC50 = 4.36 and 2.50 ¦ÌM, resp.), cell lines. Moreover, combining 5a or 6e with a histone deacetylase (HDAC) inhibitor further improved the in vitro anti-proliferation activity. Further research showed that 5a caused HGC-27 cell apoptosis by downregulating Bcl-2 and upregulating Bax. In addition, a mol. docking anal. showed that compounds 5a and 6e could bind to GRPR. In conclusion, compounds 5a and 6e are novel GRPR antagonists with potent anticancer activity. [graphic not available: see fulltext]
Medicinal Chemistry Research published new progress about 104-03-0. 104-03-0 belongs to catalysis-chemistry, auxiliary class Nitro Compound,Carboxylic acid,Benzene, name is 4-Nitrophenylacetic acid, and the molecular formula is C20H28B2O4S2, Recommanded Product: 4-Nitrophenylacetic acid.
Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia