380431-33-4

Upstream product

• 112663-43-1 3-(tert-butoxycarbonylamino)propyl methanesulfonate 
• 123-08-0 4-hydroxy-benzaldehyde 
• 58885-58-8 N-tert-butoxycarbonyl-3-aminopropanol 
• 83948-53-2 3-bromopropylamine tert-butylcarbamate 

Downstream Products

• 1428331-43-4 C₂₁H₂₇N₃O₄ 
• 1428331-41-2 C₁₈H₂₀BrN₃O₃ 
• 1163713-42-5 (3-{4-[(6-phenoxybenzothiazol-2-ylamino)methyl]phenoxy}propyl)carbamic acid tert-butyl ester 

Relevant academic research and scientific papers

A platinum prodrug conjugated with a photosensitizer with aggregation-induced emission (AIE) characteristics for drug activation monitoring and combinatorial photodynamic-chemotherapy against cisplatin resistant cancer cells

A targeted and image-guided platinum prodrug conjugated with a photosensitizer with aggregation-induced emission (AIE) characteristics was designed for real-time and in situ drug activation monitoring in cancer cells as well as combinational photodynamic-

Interlayer-Sensitized Linear and Nonlinear Photoluminescence of Quasi-2D Hybrid Perovskites Using Aggregation-Induced Enhanced Emission Active Organic Cation Layers

A concept of interlayer-sensitized photoluminescence (PL) of quasi-2D hybrid perovskite (PVK) with a π-conjugated optically interacting organic cation layer is introduced and demonstrated. A rod-shaped aggregation-induced enhanced emission (AIEE) organic

SEPARATION AND ISOLATION OF NUCLEIC ACIDS USING AFFINITY LIGANDS BOUND TO A SOLID SURFACE

A method of isolating and separating a target macromolecule, such DNA (double stranded or single stranded), RNA (double stranded or single stranded), messenger RNA, or other oligonucleotide or oligonucleoside, from a sample by binding the target macromolecule to an affinity ligand that is bound to a surface is disclosed. The method may be employed in chromatography or any other of the separation sciences.

Design, synthesis, and biological evaluation of 5-aminotetrahydroquinoline-based LSD1 inhibitors acting on Asp375

The abnormal expression of lysine-specific histone demethylase 1 (LSD1) is associated with different cancer types, and LSD1?inhibitory activity seems to have high therapeutic potential in cancer treatment. Here, we report the design, synthesis, and biochemical evaluation of novel 5-aminotetrahydroquinoline-based LSD1 inhibitors. Among them, compounds A6, A8, B1–B5, and C4 showed preferable inhibitory effects on LSD1, with IC50 = 0.19–0.82 μM. Several potent compounds were selected to evaluate their antiproliferative activity on A549 cells and MCF-7 cells with a high expression of LSD1. The potential binding modes of the compounds were revealed through molecular docking to rationalize the potency of compounds toward LSD1. Our data recognized that the 5-aminotetrahydroquinoline scaffold may serve as a starting point for developing potent LSD1 inhibitors for cancer therapy.

Leucine aminopeptidase and monoamine oxidase-activated near-infrared fluorescent probe as well as synthetic method and biological application thereof

The invention discloses a leucine aminopeptidase and monoamine oxidase-activated near-infrared fluorescent probe as well as a synthetic method and biological application thereof. The adopted syntheticmethod includes the following step: (1) synthesizing the novel leucine aminopeptidase and monoamine oxidase-activated near-infrared fluorescent probe (NML); and the biological application comprises the following step: (1) applying the probe to biological imaging and serum detection. The leucine aminopeptidase and monoamine oxidase-responsive fluorescent probe is synthesized for the first time, and the problem of low specificity of a traditional single-enzyme fluorescent probe is overcome; the fluorescent probe has near-infrared fluorescence properties, the background fluorescence signal can be effectively reduced, and the sensitivity of the probe can be improved; and the fluorescent probe has a good staining effect on living cells and high staining efficiency, and can detect cell endogenous leucine aminopeptidase and monoamine oxidase.

IMIDAZO [2, 1-F] [1, 2, 4] TRIAZIN-4-AMINE DERIVATIVES AS TLR7 AGONIST

Disclosed herein is an imidazo [2, 1-f] [1, 2, 4] triazin-4-amine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof useful as a TLR7 agonist, and a pharmaceutical composition comprising the same. Also disclosed herein is a method of treating cancer using the imidazo [2, 1-f] [1, 2, 4] triazin-4-amine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof as TLR7 agonist.

Design, synthesis and biological evaluation of tetrahydroquinoline-based reversible LSD1 inhibitors

The targeted regulation of LSD1, which is highly expressed in a variety of tumor cells, is a promising cancer therapy strategy. Several LSD1 inhibitors are currently under clinical evaluation, and most of these inhibitors are irreversible. Here, we report the design, synthesis and biochemical evaluation of novel tetrahydroquinoline-based reversible LSD1 inhibitors. Compounds 18s and 18x, which are selective to LSD1 over MAO-A/B, exhibit excellent LSD1 inhibition at the molecular levels with IC50 = 55 nM and 540 nM, respectively. The classic Lineweaver–Burk plots revealed that compound 18s could reversibly bind the LSD1 enzyme in a noncompetitive manner. Molecular docking was used to reveal the potential binding-mode of the compounds and interpret the structure-activity relationships. Furthermore, compounds 18s and 18x significantly inhibited proliferation (IC50 = 1.13 μM and 1.15 μM, respectively) and induced apoptosis in MGC-803 cells with high expression of LSD1. Compound 18x showed acceptable liver microsomal stability. Meanwhile, 18x did not appear to inhibit CYPs at 10 μM in vitro. Remarkably, the oral administration of compound 18x can inhibit the growth of MGC-803 xenograft tumors without significant side effects. Our findings suggest that tetrahydroquinoline-based LSD1 inhibitors deserve further investigation for the treatment of LSD1 overexpressing cancer.

POLYMERS AND OLIGOMERS WITH AGGREGATION-INDUCED EMISSION CHARACTERISTICS FOR IMAGING AND IMAGE-GUIDED THERAPY

A fluorophore or conjugated polymer with aggregation-induced emission characteristics useful for drug tracking and delivery, identification and labeling of biological subjects, such as cells or parts of a cell, as well as for imaging, and image-guided pho

In vitro evolution of a Friedel-Crafts deoxyribozyme

We report the in vitro selection of a single-stranded 72-nucleotide DNA enzyme (deoxyribozyme) that catalyzes a Friedel-Crafts reaction between an indole and acyl imidazole in good yield and in aqueous solvent. Appreciable Friedel-Crafts product requires addition of copper nitrate and the deoxyribozyme. We observe deoxyribozyme-mediated bond formation for both in cis and in trans Friedel-Crafts reactions.

Low molecular weight non-peptide mimics of ω-conotoxin GVIA

We report the synthesis and biological activity of a low molecular weight non-peptidic mimic of the analgesic peptide ω-conotoxin GVIA. The molecular weight of this compound presents a reduction by 193 g/mol compared to a previously reported lead. This co