Synthesis and structure-activity relationship study of water-soluble carbazole sulfonamide derivatives as new anticancer agents was written by Liu, Yonghua;Wu, Yanbin;Sun, lianqi;Gu, Yuxi;Hu, Laixing. And the article was included in European Journal of Medicinal Chemistry in 2020.Reference of 28020-37-3 This article mentions the following:
Here, the structure-activity relationships of novel N-substituted carbazole sulfonamide derivatives I [R1 = H, CH2CH2OH, 3-(1-piperidyl)propanoyl, etc.; R2 = H, OH, OP(O)(ONa)2] with improved physicochem. properties was formulated and investigated. Most of these new compounds displayed good aqueous solubility Certain mols. presented strong in vitro antiproliferative and in vivo antitumor activity. Relative to the control, 50 mg/kg compound I [R1 = CH2CH2OP(O)(ONa)2; R2 = H] substantially reduced human HepG2 xenograft mouse tumor growth by 54.5% and its efficacy was comparable to that of CA-4P. Compound I [R1 = 2-(4-methylpiperazin-1-yl)ethyl; R2 = H] demonstrated anticancer efficacy in both s.c. and orthotopic HepG2 xenograft mouse models. A novel synthetic method for 7-hydroxy-substituted carbazole sulfonamides was also developed. Compared with the control, 25 mg/kg compound I [R1 = H; R2 = OP(O)(ONa)2] inhibited human HepG2 xenograft mouse tumor growth by 71.7% and was more potent than 50 mg/kg CA-4P with only 50% tumor shrinkage efficacy. Among the three water-soluble carbazole sulfonamide derivatives formulated in the present study, compound I [R1 = H; R2 = OP(O)(ONa)2] displayed the most effective tumor growth inhibition in vivo and merit further investigation as potential antitumor agents for cancer therapy. In the experiment, the researchers used many compounds, for example, 3-Amino-2,6-dimethoxypyridine (cas: 28020-37-3Reference of 28020-37-3).
3-Amino-2,6-dimethoxypyridine (cas: 28020-37-3) belongs to pyridine derivatives. Pyridine is diamagnetic and has a diamagnetic susceptibility of â?8.7 à 10â? cm3·molâ?.The molecular electric dipole moment is 2.2 debyes. The standard enthalpy of formation is 100.2 kJ·molâ? in the liquid phase and 140.4 kJ·molâ? in the gas phase. One of the examples of pyridines is the well-known alkaloid lithoprimidine, which is an A3 adenosine receptor antagonist and N,N-dimethylaminopyridine (DMAP) analog, commonly used in organic synthesis.Reference of 28020-37-3