Structural Optimization of Indole Derivatives Acting at Colchicine Binding Site as Potential Anticancer Agents was written by Hwang, Dong-Jin;Wang, Jin;Li, Wei;Miller, Duane D.. And the article was included in ACS Medicinal Chemistry Letters in 2015.Application of 189230-41-9 This article mentions the following:
Diarylisoquinolines and (trimethoxyphenyl)(indolyl)imidazopyridines I (R = 2-indolyl, 3-indolyl, 4-indolyl, 6-indolyl, 7-indolyl), analogs of a previous trimethoxybenzoylphenylindole and I (R = 5-indolyl), were prepared as tubulin polymerization inhibitors acting at the colchicine binding site for potential use as antitumor agents with improved metabolic stabilities and cytotoxicities. I (R = 2-indolyl, 3-indolyl, 4-indolyl, 6-indolyl, 7-indolyl) inhibited tubulin polymerization with IC50 values of 3 to 175 nM against a panel of human melanoma and prostate cancer cell lines. In particular, I (R = 6-indolyl) showed improved cytotoxic potency (average IC50 of 9.75 nM vs 55.75 nM) and metabolic stability in human liver microsomes (half-life time was 56.3 min vs. 45.4 min) as compared to previously reported I (R = 5-indolyl). I (R = 6-indolyl) was effective against P-glycoprotein (P-gp) mediated multiple drug resistance (MDR) and taxol resistance. In the experiment, the researchers used many compounds, for example, 2-Bromopyridine-3,4-diamine (cas: 189230-41-9Application of 189230-41-9).
2-Bromopyridine-3,4-diamine (cas: 189230-41-9) belongs to pyridine derivatives. Pyridine’s the lone pair does not contribute to the aromatic system but importantly influences the chemical properties of pyridine, as it easily supports bond formation via an electrophilic attack. 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.Application of 189230-41-9