75257-79-3

Upstream product

• 76-83-5 trityl chloride 
• 107-15-3 ethylenediamine 
• 1357108-40-7 (9H-fluoren-9-yl)methyl N-(2-(tritylamino)ethyl)carbamate 

Downstream Products

• 324000-15-9 C₃₄H₃₈O₈ 
• 848770-85-4 5-amino-1-methyl-N-[2-(tritylamino)ethyl]-1H-pyrazole-4-carboxamide 
• 123580-02-9 1-Phenyl-1-cyclohexyl-3-(4-tritylaminobutyl)amino-1-propanol 
• 123580-00-7 1-Phenyl-1-cyclohexyl-3-(2-tritylaminoethyl)amino-1-propanol 
• 728878-17-9 N-(2-tritylaminoethyl)-4-ethynylbenzamide 
• 1415815-95-0 4-((2-(tritylamino)ethylamino)methyl)phenol 
• 1415815-96-1 4-(4-((2-(tritylamino)ethylamino)methyl)phenoxy)phthalonitrile 

Relevant academic research and scientific papers

Synthesis of an aggregation-induced emission (AIE) active salicylaldehyde based Schiff base: Study of mechanoluminescence and sensitive Zn(II) sensing

Syntheses of multi-functional Aggregation-Induced Emission (AIE) active molecules in a simple manner have been drawing great attention in current luminescence materials research. In this report a simple diamine molecule (N1-tritylethane-1,2-dia

Highly Selective Detection of H+ and OH- with a Single-Emissive Iridium(III) Complex: A Mild Approach to Conversion of Non-AIEE to AIEE Complex

A greenish-blue emissive bis-cyclometalated iridium(III) complex with octahedral geometry was synthesized in a convenient route where a bulky substituted ligand, N1-tritylethane-1,2-diamine ligand (trityl-based rotating unit) (L1), w

Comprehensive structure-activity-relationship of azaindoles as highly potent FLT3 inhibitors

Acute myeloid leukemia (AML) is characterized by fast progression and low survival rates, in which Fms-like tyrosine kinase 3 (FLT3) receptor mutations have been identified as a driver mutation in cancer progression in a subgroup of AML patients. Clinical trials have shown emergence of drug resistant mutants, emphasizing the ongoing need for new chemical matter to enable the treatment of this disease. Here, we present the discovery and topological structure-activity relationship (SAR) study of analogs of isoquinolinesulfonamide H-89, a well-known PKA inhibitor, as FLT3 inhibitors. Surprisingly, we found that the SAR was not consistent with the observed binding mode of H-89 in PKA. Matched molecular pair analysis resulted in the identification of highly active sub-nanomolar azaindoles as novel FLT3-inhibitors. Structure based modelling using the FLT3 crystal structure suggested an alternative, flipped binding orientation of the new inhibitors.

Design, Synthesis, and Evaluation of Lipopeptide Conjugates of Mercaptoundecahydrododecaborate for Boron Neutron Capture Therapy

We developed new 10B carriers for boron neutron capture therapy (BNCT) that can effectively transport and accumulate boron clusters into cells. These carriers consist of a lipopeptide, mercaptoundecahydrododecaborate (BSH), and a disulfide linker. The carriers were conceived according to the structure of pepducin, a membrane-penetrating lipopeptide targeting protease-activated receptor 1 (PAR1). To improve the membrane permeability of BSH, the structure was optimized using various lipopeptides possessing different peptides and lipid moieties. These synthesized lipopeptides were conjugated with BSH and evaluated for intracellular uptake using T98G glioblastoma cells. Among them, the most effectively incorporated and accumulated in the cells was compound 5 a, which contains a peptide of 13 residues derived from the intracellular third loop of PAR1 and a palmitoyl group. For further improvement of 10B accumulation in cells, the introduction of an amine linker was investigated; intracellular uptake similar to that of 5 a was observed for compound 14, which has a piperazine linker. Both compounds 5 a and 14 showed a stronger radiosensitizing effect than BSH along on T98G cells under mixed-neutron beam irradiation. The results demonstrate that lipopeptide conjugation is effective for enhancing intracellular delivery and accumulation of BSH and improving the cytotoxic effect of BNCT.

Efficient Delivery of Quantum Dots into the Cytosol of Cells Using Cell-Penetrating Poly(disulfide)s

Quantum dots (QDs) are extremely bright, photostable, nanometer particles broadly used to investigate single molecule dynamics in vitro. However, the use of QDs in vivo to investigate single molecule dynamics is impaired by the absence of an efficient way

A multi-amine phthalocyanine and its derivatives, their preparation and use

The invention discloses polyamine phthalocyanine and a derivative thereof. The structural general formula of the derivative of polyamine phthalocyanine is shown in descriptions. The derivative of polyamine phthalocyanine, disclosed by the invention, has r

Triphenylbutanamines: Kinesin spindle protein inhibitors with in vivo antitumor activity

The human mitotic kinesin Eg5 represents a novel mitotic spindle target for cancer chemotherapy. We previously identified S-trityl-l-cysteine (STLC) and related analogues as selective potent inhibitors of Eg5. We herein report on the development of a series of 4,4,4-triphenylbutan-1-amine inhibitors derived from the STLC scaffold. This new generation systematically improves on potency: the most potent C-trityl analogues exhibit Kiapp ≥ 10 nM and GI50 ≈ 50 nM, comparable to results from the phase II clinical benchmark ispinesib. Crystallographic studies reveal that they adopt the same overall binding configuration as S-trityl analogues at an allosteric site formed by loop L5 of Eg5. Evaluation of their druglike properties reveals favorable profiles for future development and, in the clinical candidate ispinesib, moderate hERG and CYP inhibition. One triphenylbutanamine analogue and ispinesib possess very good bioavailability (51% and 45%, respectively), with the former showing in vivo antitumor growth activity in nude mice xenograft studies.

Synthesis of novel octa-cationic and non-ionic 1,2-ethanediamine substituted zinc (II) phthalocyanines and their in vitro anti-cancer activity comparison

Novel tetra-substituted zinc phthalocyanines (Pcs) bearing 1,2-ethanediamine group and the quaternized derivatives were synthesized and characterized. The photophysical and cellular properties of these Pcs were investigated. The results indicated that the

Design, synthesis and evaluation of novel uracil acetamide derivatives as potential inhibitors of Plasmodium falciparum dUTP nucleotidohydrolase

The ubiquitous enzyme dUTP nucleotidohydrolase (dUTPase) catalyses the hydrolysis of dUTP to dUMP and can be considered as the first line of defence against incorporation of uracil into DNA. Inhibition of this enzyme results in over-incorporation of uraci

DNA METHYL TRANSFERASE INHIBITORS CONTAINING A ZINC BINDING MOIETY

The present invention relates to inhibitors of DNMT containing zinc moiety derivatives that have enhanced or unique properties as inhibitors of DNA methyl transferases (DNMT) and their use in the treatment of DNMT related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.