1301599-47-2

Upstream product

• 42268-88-2 1,3-dimethyl 5-(bromomethyl)benzene-1,3-dicarboxylate 
• 1301599-45-0 dimethyl 5-(N,N-dimethyl)aminoisophthalate 
• 181425-91-2 diethyl 5-(hydroxymethyl)isophthalate 

Downstream Products

• 1301599-51-8 1,3-bis(aminomethyl)-5-(N,N-dimethylamino)methylbenzene 
• 1301599-48-3 C₁₁H₁₅N₇ 

Relevant academic research and scientific papers

LIPIDS AND LIPID COMPOSITIONS FOR THE DELIVERY OF ACTIVE AGENTS

This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1–R4, L and X are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.

Macrocyclic pyridyl polyoxazoles: Structure-activity studies of the aminoalkyl side-chain on G-quadruplex stabilization and cytotoxic activity

Pyridyl polyoxazoles are 24-membered macrocyclic lactams comprised of a pyridine, four oxazoles and a phenyl ring. A derivative having a 2-(dimethylamino)ethyl chain attached to the 5-position of the phenyl ring was recently identified as a selective G-quadruplex stabilizer with excellent cytotoxic activity, and good in vivo anticancer activity against a human breast cancer xenograft in mice. Here we detail the synthesis of eight new dimethylamino-substituted pyridyl polyoxazoles in which the point of attachment to the macrocycle, as well as the distance between the amine and the macrocycle are varied. Each compound was evaluated for selective G-quadruplex stabilization and cytotoxic activity. The more active analogs have the amine either directly attached to, or separated from the phenyl ring by two methylene groups. There is a correlation between those macrocycles that are effective ligands for the stabilization of G-quadruplex DNA (ΔTtran 15.5-24.6 °C) and cytotoxicity as observed in the human tumor cell lines, RPMI 8402 (IC 50 0.06-0.50 μM) and KB3-1 (IC50 0.03-0.07 μM). These are highly selective G-quadruplex stabilizers, which should prove especially useful for evaluating both in vitro and in vivo mechanism(s) of biological activity associated with G-quaqdruplex ligands.