Hawash, Mohammed; Kahraman, Deniz Cansen; Ergun, Sezen Guntekin; Cetin-Atalay, Rengul; Baytas, Sultan Nacak published the artcile< Synthesis of novel indole-isoxazole hybrids and evaluation of their cytotoxic activities on hepatocellular carcinoma cell lines>, Quality Control of 3731-53-1, the main research area is indole isoxazole carboxamide preparation antitumor activity physicochem property; Apoptosis; CDK4; Cell cycle arrest; Hepatocellular carcinoma; Indole; Isoxazole.
In this study, a series of indole-3-isoxazole-5-carboxamide derivatives I (R = n-butylamine, 3,4,5-(trimethoxyphenyl)aminyl, morpholin-4-yl, etc.) was designed, synthesized, and evaluated for their anticancer activities. The cytotoxic activity was performed against Huh7, MCF7 and HCT116 cancer cell lines using sulforhodamine B assay. Some compounds I showed potent anticancer activities and three of them were chosen for further evaluation on liver cancer cell lines based on SRB assay and real-time cell growth tracking anal. Compounds I were shown to cause arrest in the G0/G1 phase in Huh7 cells and caused a significant decrease in CDK4 levels. A good correlation was obtained between the theor. predictions of bioavailability using Molinspiration calculation, Lipinski’s rule of five, and exptl. verification. These investigations reveal that indole-isoxazole hybrid system have the potential for the development of novel anticancer agents.
BMC Chemistry published new progress about Amides Role: PAC (Pharmacological Activity), PRP (Properties), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), PREP (Preparation), USES (Uses). 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Quality Control of 3731-53-1.