341036-35-9

Upstream product

• 369-36-8 6-fluoro-3-nitroaniline 
• 13250-46-9 acetyl isothiocyanate 
• 1147550-11-5 ammonium thiocyanate 

Downstream Products

• 100817-91-2 2-acetylamino-5-nitro-1,3-benzothiazole 
• 73458-39-6 5-nitro-benzothiazol-2-ylamine 

Relevant academic research and scientific papers

2,5- and 2,6-disubstituted benzazole derivatives useful as protein kinase inhibitors

The present invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, wherein the substituent is attached to the 5- or 6- position of the benzazole; Xindependently represents S, O, SO, SO2;Yindependently represents S, O, NR2, SO, SO2;Aindependently represents ←CO-, ←CS-, ←SO-, ←SO2-, ←CO2-, ←CONR8-, ←NR8CO-, ←NR8CONR9-, ←NR8COO-, ←NR8NR9CO-, ←NR8OCO-, ←ONR8CO-, ←NR8SO2-, where ← indicates the point of attachment to R3; and wherein R1 to R19 in formula (I) represent independently of each other a variety of different substituents comprising alkyl, aryl, aralkyl, alkylaryl, heteroaryl groups and monofunctional moieties. These compounds are useful as protein kinase inhibitors in the treatment of i.a. cancer.

Benzazole analogues and uses thereof

The present invention relates to N2-heteroaryl-benzazole-2,(5 or 6)-diamine derivatives and compositions thereof as protein kinase inhibitors for the treatment of e.g. cancer.

2,5- and 2,6-disubstituted benzazole analogues useful as protein kinase inhibitors

The present invention relates to compounds of the general formulas (I), (Ia) and (II) and salts and physiologically functional derivatives thereof, wherein the substituents -Y are attached to the 5- or 6- position of the benzazole. These compounds are useful as protein kinase inhibitors in the treatment of i.a. cancer.

Benzazole analogues and uses thereof

The present invention relates to compounds of the general formulas (I), (Ia) and (II) and salts and physiologically functional derivatives thereof, wherein the substituents —Y are attached to the 5- or 6-position of the benzazole.

Synthesis and biological evaluation of benzothiazole derivatives as potent antitumor agents

Based on 2-methyl-4-nitro-2H-pyrazole-3-carboxylic acid[2- (cyclohexanecarbonylamino)benzothiazol-6-yl]amide (1), which shows selective cytotoxicity against tumorigenic cell lines, 2,6-dichloro-N-[2- (cyclopropanecarbonylamino)benzothiazol-6-yl]benzamide (13b) was designed and synthesized as a biologically stable derivative containing no nitro group. The highly potent derivative 13b exhibited excellent in vivo inhibitory effect on tumor growth.

Kinetics and mechanism of methanolysis and cyclization of 1-acyl-3-(2-halo-5-nitrophenyl)thioureas

The kinetics of methoxide ion-catalysed solvolysis of 1-acyl-3-(2-halo-5-nitrophenyl)thioureas and cyclization of fluoro derivatives were studied in methanol at 25 deg C. The cyclization involved the substitution of fluorine by sulphur anion of thiourea and proceeded in two steps. With the acetyl derivative, the first step is methanolysis and the second step is much slower cyclization of the 2-fluoro-5-nitrophenylthiourea anion formed to give 2-amino-5-nitro-1,3-benzothiazole. With the benzoyl derivative, the first step involves parallel methanolysis of the benzoyl group and cyclization to 2-benzoylamino-5-nitro-1,3-benzothiazole. At concentrations of sodium methoxide higher than ca. 0.01 mol l-1 the rates of solvolyses of all the acyl halothioureas decreased and at concentrations higher than ca. 0.01 mol l-1 the rates of solvolyses of all the acyl halothioureas decreased and at concentrations higher than ca. 0.4 mol l-1 there was an increase in the formation of other product(s) than the product of cyclization. After the addition of 18-crown-6, the side products were not formed and the cyclization of fluoro derivatives were considerably accelerated. The slowing of the solvolytic reaction and acceleration of the cyclization reaction are most probably due to the formation of dianions.