Novel trityl linked drug immunoconjugates for cancer therapy

Synthesis and in vitro Modeling and Characterization of Self-AssemblingDrug Conjugates for Targeted Medicinal Application

“…A number of diverse yet cogent strategies are available to increase the efficacy of the API and drug delivery form [6,9,10,50,56,62]. The extent and applicability of various forms of pro-drug format varies considerably.…”

“…Typically aggregates must accommodate moieties from conjugation of a number of organic entities [9,15,27,[37][38][39] with ease. A complex conjugate of particular activity has been described based on attachment to an immuno-responsive agent [9]. In this case it carried with it particular difficulties of component compatibility and obfuscation.…”

“…Organic conjugates of formulation aids, associated drugs and chemical entities such as technetium, 99 Tc, used in radiotherapy [5] are used ubiquitously in medicine for diagnosis and as surgical aids. Medicinal applications include chemotherapy [6][7][8][9][10] when isotopes can be used as light particle emitters and localized miniaturized thermal devices, some such applications were recently discovered for labeled gold particles. In the case of imaging, conjugated drugcarriers have been used in medicine for utilization in radioopacity or magnetic resonance (spectroscopic) imaging applications [11,12].…”

Unusual Stability of Diastereomers of the Isomeric Pyridine-based Leuco-TAM Dyes 2,2'-(2-(Pyridin-4 or 3-yl)propane-1,3-diylidene)bis(5-chloro-1,3,3-trimethylindoline)

“…This use of trityl groups is particularly common in multistep solid-phase syntheses, mostly as linkers. 13,14 Trityl cations can also act as a tool for a mass-spectrometric analysis because of their easy ionization.…”

“…13,14 All of the pyridine-based LTAM molecules 1-3 were obtained as yellowish-white powders. For comparison, a p-nitro derivative 4 was also prepared similarly via the reaction of substituted FB and p-nitrobenzaldehyde.…”