91538-55-5

Upstream product

• 40357-96-8 5-nitro-thiophene-3-carboxylic acid 

Downstream Products

• 127648-96-8 1-methyl-2(2'-nitro-4'-thienylcarboxamido)-methyl-5(2'-fluorophenyl)-2H-1,4-benzodiazepine 
• 36050-09-6 5-nitrothiophene-3-carboxamide 
• 1255908-05-4 benzyl N,N'-di(5-nitrothien-3-ylcarbonyl)-imidoselenocarbamate 
• 956830-56-1 5-aminothiophene-3-carboxylic acid [2,6-dimethyl-4-(1,2,2,2-tetrafluoro-1-trifluoromethylethyl)phenyl]amide 
• 956830-52-7 5-nitrothiophene-3-carboxylic acid [2,6-dimethyl-4-(1,2,2,2-tetrafluoro-1-trifluoromethylethyl)phenyl]amide 

Relevant academic research and scientific papers

Benzoylurea derivatives as a novel class of antimitotic agents: Synthesis, anticancer activity, and structure-activity relationships

Forty-six new compounds were synthesized on the basis of our knowledge of the 3-haloacylamino benzoylurea (HBU) series. Structure-activity relationship (SAR) analysis indicates that (i) the configuration of the chiral center in 1 (JIMB01) is not indispensable for the activity, (ii) the phenyl ring is essential, and (iii) a substitution at the 6-position of the phenyl ring with a halogen enhances the activity. Among the analogues, 11e and 14b bearing 6-fluoro substitution showed potent activities against nine human tumor cell lines, including CEM (leukemia), Daudi (lymphoma), MCF-7 (breast cancer), Bel-7402 (hepatoma), DU-145 (prostate cancer), PC-3 (prostate cancer), DND-1A(melanoma), LOVO (colon cancer), and MIA Paca (pancreatic cancer) with IC50 values between 0.01 and 0.30 μM. 14b inhibited human hepatocarcinoma by 86% in volume in nude mice. The mechanism of 14b is to inhibit microtubule assembly, followed by the M-phase arrest, bcl-2 inactivation, and then apoptosis. We consider 14b promising for further anticancer investigation.

INSECTICIDAL COMPOUNDS

Novel heteroaromatic compounds of formula (I): wherein A1, A2, A3, R1, R2, G1, G2, Q1 and Q2 are as defined in claim 1; or salts or N-oxides thereof. Furthe

Opioid ligands related to tifluadom

In an effort to prepare ligands with kappa selective affintity suitable for use in affinity chromatography, we synthesized the haloacetamido derivatives 17 and 18 of tifluadom.These compounds showed modest opioid binding affinity but were more active at the mu than at the kappa site.The nitro compounds 7 and 16 were prepared as potential intermediates.The former, a weak mu agonist, was devoid of kappa affinity (IC50 > 1E-6 M), whereas the latter was a mu selective agonist.Keywords: tifluadom/ benzodiazepines/ affinity chromathography/ opioid binding activity

Secondary Steric Effects in Piperidinodebromination of Some 2-Bromo-4-R-5-nitrothiophene-3-carboxamides in Methanol

The rates of piperidinodebromination of some N-substituted 2-bromo-4-R-5-nitrothiophene-3-carboxamides (R = H and Me) have been measured in methanol.The kinetic data obtained, as well as the investigation of the restricted rotation about the C-N bond of the amino group of some of the above carboxamides by dynamic n.m.r. spectroscopy, have shown the occurrence of steric interactions which force the 3-carboxamido group to rotate about its bond with the aromatic ring.This causes a reduced activation and a kinetic secondary steric effect.

Synthesis of Isomeric β-Haloethylthienopyrroles

The preparation of ethyl 4-(2-bromoethyl)thienopyrrole-5-carboxylate and ethyl 6-(2-bromoethyl)thienopyrrole-5-carboxylate by reaction of t-butyl 2-(2-thienyl)carbazate and t-butyl 2-(3-thienyl)carbazate with ethyl-5-bromo-2-oxopentanoate are described.