3125-63-1

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Uses

Antifungal activity of 3-?Isothiocyanatophenol was studied.

Upstream product

• 463-71-8 thiophosgene 
• 591-27-5 m-Hydroxyaniline 
• 1414781-35-3 C₇H₇NOS₂*C₆H₁₂N₂ 
• 75-44-5 phosgene 

Downstream Products

• 3394-05-6 N-(3-hydroxyphenyl)thiourea 
• 875244-00-1 3-allyloxy-phenyl isothiocyanate 
• 1350545-16-2 8-(3-hydroxyphenylamino)-9-cyclopentyl-2-(4-(4-methylpiperazin-1-yl)phenylamino)-9H-purine 
• 62950-66-7 1-(2-chloroallyl)-1-dodecyl-3-[3'-(N-methylcarbamoyloxy)phenyl] urea 
• 116986-58-4 5-Amino-3-morpholin-4-yl-[1,2,4]triazole-1-carbothioic acid (3-hydroxy-phenyl)-amide 
• 109285-57-6 4-methyl-piperazine-1-carbothioic acid-(3-hydroxy-anilide) 

Relevant academic research and scientific papers

Synthesis of 2-substituted tetrahydroisoquinolin-6-ols: Potential scaffolds for estrogen receptor modulation and/or microtubule degradation

6-Methoxytetrahydroisoquinoline hydrochloride was converted into four small libraries of substituted ureas, thioureas, sulfonamides and N-aryls, using the tetrahydroisoquinoline nitrogen as the scaffold-linking atom. Some of the compounds were evaluated for their ability to inhibit cell proliferation using the MCF7 (invasive ductal carcinoma) cell line.

Structural optimization and structure-activity relationships of N 2-(4-(4-methylpiperazin-1-yl)phenyl)- N 8-phenyl-9 H -purine-2,8-diamine derivatives, a new class of reversible kinase inhibitors targeting both EGFR-activating and resistance mutations

This paper describe the structural optimization of a hit compound, N 2-(4-(4-methylpiperazin-1-yl)phenyl)-N8-phenyl-9H-purine- 2,8-diamine (1), which is a reversible kinase inhibitor targeting both EGFR-activating and drug-resistance (T790M) mutations but has poor binding affinity. Structure-activity relationship studies led to the identification of 9-cyclopentyl-N2-(4-(4-methylpiperazin-1-yl)phenyl)-N 8-phenyl-9H-purine-2,8-diamine (9e) that exhibits significant in vitro antitumor potency against the non-small-cell lung cancer (NSCLC) cell lines HCC827 and H1975, which harbor EGFR-activating and drug-resistance mutations, respectively. Compound 9e was further assessed for potency and selectivity in enzymatic assays and in vivo anti-NSCLC studies. The results indicated that compound 9e is a highly potent kinase inhibitor against both EGFR-activating and resistance mutations and has good kinase spectrum selectivity across the kinome. In vivo, oral administration of compound 9e at a dose of 5 mg/kg caused rapid and complete tumor regression in a HCC827 xenograft model, and an oral dose of 50 mg/kg initiated a considerable antitumor effect in an H1975 xenograft model.