Yu, Ming-jun; Li, Chao; He, Meng; Zhu, Yu-ting; Yang, Rui; Deng, Sheng-song; Meng, Xiao-ming; Yao, Ri-sheng published their research in Medicinal Chemistry Research in 2021. The article was titled 《Structure-activity relationship studies on Pd176252 derivatives leading to discovery of novel GRP receptor antagonist with potent anticancer activity》.HPLC of Formula: 7524-52-9 The article contains the following contents:
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 μM, resp.), Pan02 (IC50 = 4.36 and 2.50 μM, resp.), and HGC-27 (IC50 = 4.36 and 2.50 μM, 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]H-Trp-OMe.HCl(cas: 7524-52-9HPLC of Formula: 7524-52-9) was used in this study.
H-Trp-OMe.HCl(cas:7524-52-9) is one of amino acid derivatives. Amino acid derivatives represent an important category of skin penetration promoters. These compounds possess hydrophobic chains attached to an amino acid headgroup via a biodegradable ester bond. Due to the amphiphilic nature of these derivatives, it is possible for them to enter into the SC lipid barrier and significantly disorganize skin membrane lipids.HPLC of Formula: 7524-52-9
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