5006-69-9

Usage

Uses

Used in Pharmaceutical Industry:
Zinc03944768 is used as a key intermediate in the synthesis of next-generation hypoxic tumor cell radiosensitizers. These radiosensitizers are designed to enhance the effectiveness of radiation therapy in cancer treatment, particularly for hypoxic (oxygen-deficient) tumor cells that are resistant to conventional radiation therapy. The presence of the nitro group in the compound allows for the generation of reactive nitrogen species upon exposure to radiation, which can increase the radiosensitivity of hypoxic tumor cells and improve the overall therapeutic outcome.
Additionally, the ethyl and hydroxyl groups in Zinc03944768 may contribute to its solubility and stability, making it a suitable candidate for further chemical modifications and optimization to develop more effective and targeted radiosensitizers. Zinc03944768 can also be used as a starting material for the synthesis of other bioactive molecules with potential applications in various therapeutic areas.

Upstream product

• 3034-38-6 1H-4⁽⁵⁾-nitroimidazole 
• 540-51-2 2-bromoethanol 
• 13230-21-2 (4-nitro-imidazol-1-yl)-acetic acid methyl ester 

Downstream Products

• 930100-32-6 C₁₈H₂₂F₂N₄O₃ 
• 1447794-56-0 N-[5-[[3-cyano-7-[[1-(2-hydroxyethyl)imidazol-4-yl]amino]pyrazolo[1,5-a]pyrimidin-5-yl]amino]-2-methylphenyl]acetamide 

Relevant academic research and scientific papers

Artemisinin-indole and artemisinin-imidazole hybrids: Synthesis, cytotoxic evaluation and reversal effects on multidrug resistance in MCF-7/ADR cells

A series of artemisinin derivatives with MDR reversal activity were designed and synthesized. All hybrids were screened to anticancer activities against four human cancer cell lines (A549, MCF-7, HepG-2, MDA-MB-231) and normal human hepatic cell (L02) in vitro. Most of the new compounds showed higher anticancer activities than artemisinin, among which compounds 11a and 11c displayed superior potency with IC50 6.78 μM and 5.25 μM against MCF-7, respectively. The further research indicated that the most potent 11c induced cell cycle arrest at G2 phase in MCF-7. Additionally, compound 11c showed remarkable MDR reversal activity which reversed adriamycin against MCF-7/ADR cells with IC50 0.76 μM.

Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides

Innovations in the field of radiotherapy such as stereotactic body radiotherapy, along with the advent of radio-immuno-oncology, herald new opportunities for classical oxygen-mimetic radiosensitizers. The role of hypoxic tumor cells in resistance to radiotherapy and in suppression of immune response continues to endorse tumor hypoxia as a bona fide, yet largely untapped, drug target. Only nimorazole is used clinically as a radiosensitizer, and there is a dearth of new radiosensitizers in development. Here we present a survey of novel nitroimidazole alkylsulfonamides and document their cytotoxicity and ability to radiosensitize anoxic tumor cells in vitro. We use a phosphate prodrug approach to increase aqueous solubility and to improve tumor drug delivery. A 2-nitroimidazole and a 5-nitroimidazole analogue demonstrated marked tumor radiosensitization in either ex vivo assays of surviving clonogens or tumor regrowth delay.

Diamide amino-imidazoles: A novel series of γ-secretase inhibitors for the treatment of Alzheimers disease

The synthesis and structure-activity relationship (SAR) of a novel series of di-substituted imidazoles, derived from modification of DAPT, are described. Subsequent optimization led to identification of a highly potent series of inhibitors that contain a β-amine in the imidazole side-chain resulting in a robust in vivo reduction of plasma and brain Aβ in guinea pigs. The therapeutic index between Aβ reductions and changes in B-cell populations were studied for compound 10h.