Recently I am researching about BIOLOGICAL EVALUATION; ANTITUMOR-ACTIVITY; DERIVATIVES BEARING; MULTIKINASE INHIBITOR; CLICK CHEMISTRY; DESIGN; CANCER; DISCOVERY; MOIETY; METASTASIS, Saw an article supported by the Institute for the Promotion of Teaching Science and Technology (IPST) [19/2558]; The Thailand Research FundThailand Research Fund (TRF) [RTA6280004]; Department of Chemistry, Faculty of Science, Silpakorn University; Center of Excellence in Hepatitis and Liver Cancer, Department of Biochemistry, Faculty of Medicine, Chulalongkorn University. Published in ACADEMIC PRESS INC ELSEVIER SCIENCE in SAN DIEGO ,Authors: Palakhachane, S; Ketkaew, Y; Chuaypen, N; Sirirak, J; Boonsombat, J; Ruchirawat, S; Tangkijvanich, P; Suksamrarn, A; Limpachayaporn, P. The CAS is 150-76-5. Through research, I have a further understanding and discovery of Mequinol. Safety of Mequinol
A series of 1,2,3-triazole-containing Sorafenib analogues, in which the aryl urea moiety of Sorafenib (1) was replaced with a 1,2,3-triazole ring linking a substituted phenoxy fragment, were prepared successfully via Huisgen 1,3-dipolar cycloaddition and nucleophilic aromatic substitution. The studies of cytotoxicity towards human hepatocellular carcinoma (HCC) cell lines, HepG2 and Huh7, indicated that p-tert-butylphenoxy analogue 2m showed significant inhibitory activity against Huh7 with IC50 = 5.67 +/- 0.57 mu M. More importantly, 2m showed low cytotoxicity against human embryonal lung fibroblast cell line, MRC-5, with IC50 > 100 mu M, suggesting its highly selective cytotoxic activity (SI > 17.6) towards Huh7 which is much superior to that of Sorafenib (SI = 6.73). The molecular docking studies revealed that the analogue 2m bound B-RAF near the binding position of Sorafenib, while it interacted VEGFR2 efficiently at the same binding position of Sorafenib. However, 2m exhibited moderate inhibitory activity toward B-RAF, implying that its anti-Huh7 effect might not strictly relate to inhibition of B-RAF. Wound healing and BrdU cell proliferation assays confirmed anti-cell migration and anti-cell proliferative activities towards Huh7. With its inhibitory efficiency and high safety profile, 2m has been identified as a promising candidate for the treatment of HCC.
Safety of Mequinol. Welcome to talk about 150-76-5, If you have any questions, you can contact Palakhachane, S; Ketkaew, Y; Chuaypen, N; Sirirak, J; Boonsombat, J; Ruchirawat, S; Tangkijvanich, P; Suksamrarn, A; Limpachayaporn, P or send Email.
Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles