372198-70-4

Usage

Type of compound

Thiourea derivative

Structural features

Benzene ring
Methyl group (-CH3) attached to the benzene ring
Nitro group (-NO2) attached to the benzene ring

Potential applications

Pharmaceuticals
Agrochemicals

Reactivity

May pose risks to health and the environment

Safety concerns

Handle with caution due to potential toxicity

Further research

Necessary to fully understand safety and potential uses

Upstream product

• 300819-83-4 C₁₅H₁₃N₃O₃S 

Downstream Products

• 21352-59-0 2,7-bis-(2-methyl-5-nitro-anilino)-1,6-dithia-3,8-diaza-spiro[4.4]nona-2,7-diene-4,9-dione 
• 1143459-81-7 N-(2-methyl-5-nitrophenyl)-4-(pyridin-3-yl)thiazol-2-amine hydrobromide 

Relevant academic research and scientific papers

Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: A series of Imatinib hybrides as potent Inhibitors of wild-type and mutant BCR-ABL, PDGF-Rβ, and histone deacetylases

Inhibitors of histone deacetylases are a new class of cancer therapeutics with possibly broad applicability. Combinations of HDAC inhibitors with the kinase inhibitor 1 (Imatinib) in recent studies showed additive and synergistic effects. Here we present a new concept by combining inhibition of protein kinases and HDACs, two independent pharmacological activities, in one synthetic small molecule. In general, the HDAC inhibition profile, the potencies, and the probable binding modes to HDAC1 and HDAC6 were similar as for 6 (SAHA). Inhibition of Abl kinase in biochemical assays was maintained for most compounds, but in general the kinase selectivity profile differed from that of 1 with nearly equipotent inhibition of the wildtype and the Imatinib resistant Abl T315I mutant. A potent cellular inhibition of PDGFR and cytotoxicity toward EOL-1 cells, a model for idiopathic hypereosinophilic syndrome (HES), are restored or enhanced for selected analogues (12b, 14b, and 18b). Cytotoxicity was evaluated by using a broad panel of tumor cell lines, with selected analogues displaying mean IC50 values between 3.6 and 7.1 μM.

NOVEL BIFUNCTIONAL COMPOUNDS WHICH INHIBIT PROTEIN KINASES AND HISTONE DEACETYLASES

The present invention relates to a bifunctional compound of formula I or its pharmaceutically acceptable salts or solvates A-L-B (I) wherein A is a histone deacetylase (HDAC) inhibitory moiety, L is a single bond or a linker group and B is a protein kinase inhibitory moiety. The bifunctional compound according to formula (I) is useful for the treatment of malignant and non-malignant neoplasia and diseases related to abnormal cell growth