79070-65-8

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General Description

1H-Benz(de)isoquinoline-1,3(2H)-dione, 2-(2-hydroxyethyl)-5-nitro- is a chemical compound with the molecular formula C16H12N2O5. It is a derivative of isoquinoline and contains a nitro group and a hydroxyethyl group. 1H-Benz(de)isoquinoline-1,3(2H)-dione, 2-(2-hydroxyethyl)-5-nitro- has potential pharmaceutical applications due to its structure, as it may have biological activity related to its interaction with biological systems. It could be used in the development of new drugs or pharmaceutical products. However, further research and studies are needed to determine the specific properties and potential uses of this chemical.

InChI:InChI=1/C14H10N2O5/c17-5-4-15-13(18)10-3-1-2-8-6-9(16(20)21)7-11(12(8)10)14(15)19/h1-3,6-7,17H,4-5H2

Upstream product

• 3027-38-1 3-nitro-1,8-naphthalic anhydride 
• 141-43-5 ethanolamine 

Relevant academic research and scientific papers

A two-step synthesis of medicinally-important 1,8-naphthalimide peptidyls by solid phase organic synthesis

A new approach for a short synthesis of novel medicinally-important mono-, bis- and tris-1,8-naphthalimide peptidyl derivatives is described. The method generates efficiently 1,8-naphthalimides with variable spacer lengths and charged, polar or hydrophobi

Design, synthesis, and identification of a novel napthalamide-isoselenocyanate compound NISC-6 as a dual Topoisomerase-IIα and Akt pathway inhibitor, and evaluation of its anti-melanoma activity

Synthesis and anti-melanoma activity of novel naphthalimide isoselenocyanate (NISC) and naphthalimide selenourea (NSU) analogs are described. The novel agents were screened for growth inhibition of different human melanoma cell lines including those having BRAFV600E mutation (UACC903, 1205Lu, and A375M) and BRAFWT (CHL-1). In general, the NISC analogs (4a-d) were more effective in inhibiting the cell viability than the NSU analogs (7a-b). Overall, NISC-6 (4d), having a six-carbon alkyl chain, was identified as the most cytotoxic compound in both BRAFV600E mutated and BRAFWT cells. NISC-6 docked strongly into the binding sites of Akt1 and human topoisomerase IIα (Topo-IIα), and the docking results were supported by experimental findings showing NISC-6 to inhibit of both Akt pathway and Topo-IIα activity in a dose dependent manner. Furthermore, NISC-6 effectively induced apoptosis in human melanoma cells, inhibited tumor growth by ～69% in a melanoma mouse xenograft model, and showed excellent compliance with the Lipinski’ rule of five, suggesting both its efficacy and drug-like behavior under physiological conditions.

Development of novel naphthalimide derivatives and their evaluation as potential melanoma therapeutics

Synthesis and anti-melanoma activity of various naphthalimide analogs, rationally modified by introducing isothiocyanate (ITC) and thiourea (TU) functionalities, found in well-known anti-cancer agents, is described. The structure-activity relationship comparison of the novel agents in inhibiting cancer cell growth was evaluated in various melanoma cell lines. Both ITC and TU analogs effectively inhibited cell viability and induced apoptosis in various human melanoma cells. Nitro substitution and increase in alkyl chain length, in general, enhanced the apoptotic activity of ITC derivatives. All the new compounds were well tolerated when injected intraperitoneal (i.p.) in mice at effective doses at which both the ITC and TU derivatives inhibited melanoma tumor growth in mice following i.p. xenograft. The nitro substituted naphthalimide-ITC derivative 3d was found to be the most effective in inducing apoptosis, and in inhibiting melanoma cell and tumor growth.

Small molecule modifiers of MicroRNA miR-122 function for the treatment of hepatitis C Virus infection and hepatocellular carcinoma

MicroRNAs are a recently discovered new class of important endogenous regulators of gene function. Aberrant regulation of microRNAs has been linked to various human diseases, most importantly cancer. Small molecule intervention of microRNA misregulation h

NOVEL SUBSTITUTED 1H-BENZ [DE] ISOQUINOLINE-1, 3 -DIONES

The present invention relates to novel substituted 1H-benz[de]isoquinoline-1,3-diones. This invention particularly relates to novel substituted 1H-benz[de]isoquinoline-1,3-diones particularly N-[2-(Chloroethyl)]- and N-[3-(Chloropropyl)]-naphthalimides and antitumor activity thereof. The present invention also relates to process of preparation of novel substituted 1H-benz[de]isoquinoline-1,3-diones. The present invention further relates to pharmaceutical composition for the treatment of cancer and related diseases.

ANTIBODY DRUG CONJUGATES AND METHODS

The invention relates to antibody drug conjugate (ADC) compounds represented by Formula:(I) where one or more 1,8 bis-naphthalimide drug moieties (D) having Formulas (IIa) and (Ilb)are covalently linked by a linker (L) to an antibody (Ab). The invention a