13141-88-3

Upstream product

• 2733-41-7 4-nitrobenzoyl azide 
• 95-53-4 o-toluidine 
• 619-50-1 4-nitrobenzoic acid methyl ester 
• 636-97-5 N-amino-(4-nitrophenyl)carboxamide 
• 614-68-6 2-tolyl isocyanate 
• 100-01-6 4-nitro-aniline 
• 100-28-7 4-Nitrophenyl isocyanate 

Downstream Products

• 202874-38-2 N-(4-aminophenyl)-N'-(2-methylphenyl)urea 

Relevant academic research and scientific papers

Discovery of N-phenyl-(2,4-dihydroxypyrimidine-5-sulfonamido) phenylurea-based thymidylate synthase (TS) inhibitor as a novel multi-effects antitumor drugs with minimal toxicity

Thymidylate synthase (TS) is a hot target for tumor chemotherapy, and its inhibitors are an essential direction for anti-tumor drug research. To our knowledge, currently, there are no reported thymidylate synthase inhibitors that could inhibit cancer cell migration. Therefore, for optimal therapeutic purposes, combines our previous reports and findings, we hope to obtain a multi-effects inhibitor. This study according to the principle of flattening we designed and synthesized 18 of N-phenyl-(2,4-dihydroxypyrimidine-5-sulfonamido)phenyl urea derivatives as multi-effects inhibitors. The biological evaluation results showed that target compounds could significantly inhibit the hTS enzyme, BRaf kinase and EGFR kinase activity in vitro, and most of the compounds had excellent anti-cell viability for six cancer cell lines. Notably, the candidate compound L14e (IC50 = 0.67 μM) had the superior anti-cell viability and safety to A549 and H460 cells compared with pemetrexed. Further studies had shown that L14e could cause G1/S phase arrest then induce intrinsic apoptosis. Transwell, western blot, and tube formation results proved that L14e could inhibit the activation of the EGFR signaling pathway, then ultimately achieve the purpose of inhibiting cancer cell migration and angiogenesis in cancer tissues. Furthermore, in vivo pharmacology evaluations of L14e showed significant antitumor activity in A549 cells xenografts with minimal toxicity. All of these results demonstrated that the L14e has the potential for drug discovery as a multi-effects inhibitor and provides a new reference for clinical treatment of non-small cell lung cancer.

Pyrimidine phenylurea anti-tumor compound and preparation method and application thereof

The invention belongs to the field of medicines, and particularly relates to a pyrimidine phenylurea anti-tumor compound and a preparation method and application thereof. A structure general formula of the pyrimidine phenylurea anti-tumor compound is spec

USE OF DDX3 INHIBITORS AS ANTIPROLIFERATIVE AGENTS

The present invention refers to compounds of formula I or II endowed with DDX3 inhibitory activity, relative pharmaceutical compositions and their use as antihyperproliferative agents. (I) or (II)

HUMAN HELICASE DDX3 INHIBITORS AS THERAPEUTIC AGENTS

The present invention refers to compounds endowed with RNA helicase DDX3 inhibitory activity of formula I and II and their therapeutic use, in particular for the treatment of viral diseases.

Synthesis and in vitro antiproliferative activity of novel pyrazolo[3,4-d]pyrimidine derivatives

A novel series of pyrazolo[3,4-d]pyrimidine derivatives were designed, synthesized and evaluated for their antiproliferative activity. Among the five compounds selected by NCI, compound 11a showed a distinctive pattern of selectivity on cell line panels and was further screened for a 5-log dose range, where it showed potent antiproliferative activity with median growth inhibition (GI50) equal to 1.71 μM against the CNS cancer SNB-75 cell line. The tested derivative showed remarkably the highest cell growth inhibition against non-small cell lung cancer HOP-62, CNS cancer SNB-75, breast cancer HS578T, and melanoma MALME-3M cell lines. Flow cytometric analysis revealed that compound 11a could significantly induce apoptosis in A549 cells in vitro at low micromolar concentrations. Further investigation showed that compound 11a induced significant cell cycle arrest at G0/G1 phase partly due to its ability to downregulate cyclin D1 and upregulate p27kip1 levels.

Antiproliferative effects of novel urea derivatives against human prostate and lung cancer cells; And their inhibition of β-glucuronidase activity

Twenty-one novel urea derivatives were synthesized and their structures characterized by mass, NMR, IR, and UV spectroscopy. These compounds were evaluated for their antiproliferative profile against human PC-3 (prostate) and NCI-H460 (lung) cancer cell lines. Among them, compound 21 N-(3-nitrophenyl)- N′-(1-phenylethyl)urea was found to be active against both PC-3 (IC 50 ± SEM: 20.13 ± 0.91 μM) and NCI-H460 (GI 50: 22 ± 2.6 μM) cell lines; hence has the potential to be further studied as anticancer agent. These compounds were also investigated for their ability to inhibit urease, β-glucuronidase, and phosphodiesterase enzymes. N-(2,6-Dimethylphenyl)-N′-(4′-nitrophenyl)urea (1) demonstrated 90 % inhibition of β-glucuronidase enzyme (IC50 ± SEM: 3.38 ± 0.043 μM).

Controlling molecular tautomerism through supramolecular selectivity

We have isolated the stable as well as the metastable tautomers of 1-deazapurine in the solid state by exploiting principles of supramolecular selectivity in the context of cocrystal design.

1,3-disubstituted ureas as antiglycating agents

Twenty one (21) 1,3-disubstituted urea derivatives were screened for their antiglycating potential and some of them displayed promising activity. Compound N-butyl-N'-(4-nitrophenyl)urea (6) and Nisopropyl-N'-(4-nitrophenyl)urea (18) exhibited excellent activity and could be investigated in search of medicines treating diabetes and associated complications.