165682-91-7

Upstream product

• 70-23-5 ethyl Bromopyruvate 
• 2646-30-2 1-(4-bromophenyl)thiourea 
• 617-35-6 2-oxo-propionic acid ethyl ester 

Downstream Products

• 165682-80-4 2-(4-bromophenylamino)thiazole-4-carboxylic acid 
• 1592875-28-9 2-(4-bromophenylamino)-N-methoxy-N-methylthiazole-4-carboxamide 
• 1592875-31-4 N-methoxy-N-methyl-2-(4-tributylstannylphenylamino)thiazole-4-carboxamide 
• 1592875-35-8 (2-(4-tributylstannylphenylamino)thiazol-4-yl)(3,4,5-trimethoxyphenyl)methanone 

Relevant academic research and scientific papers

Synthesis and cellular uptake of p-[123I]-phenyl-amino-thiazole (123I-PAT) as a potential agent for targeting tubulin polymerization in tumors

The phenyl-amino-thiazole (PAT) templates of methoxylbenzoyl-aryl-thiazole are potent agents against cancer by inhibiting tubulin polymerization in the nanomolar range. Herein, a radioiodinated PAT, [123I]-PAT 1, was prepared via a tributylstannyl precursor and [123I]iodide through electrophilic aromatic radioiodination. Radiolabelling of [123I]-PAT 1 was achieved in less than 15 min, with a radiochemical purity of over 99%. The accumulated radioactivity in tumor cellular uptake experiments suggested that [123I]-PAT could serve as a potential radioprobe for targeting tumor cells. Copyright

Solvent-free synthesis of bacillamide analogues as novel cytotoxic and anti-inflammatory agents

Synthesis of fourteen analogues of bacillamide, a bioactive tryptamide alkaloid of marine origin, has been accomplished through a highly efficient convergent route. The present solvent-free protocol involves the formation of thiazole ring in the initial step followed by amide coupling between substituted ethyl 2-alkyl/aryl/heteroaryl/amino/aminoarylthiazole-4-carboxylates and tryptamine in presence of 2-hydroxy-4,6-dimethylpyrimidine, a solid phase catalyst to yield N-[2-(1H-indol-3-yl)ethyl]-2-alkyl/aryl/heteroaryl/amino/aminoarylthiazole-4-carboxamides as bacillamide analogues having structural variation at position-2 of thiazole ring. Bacillamide and its analogues were evaluated for their cytotoxic activity against three cancer cell lines (HCT-116, MDA-MD-231 and JURKAT cell lines) using colorimetric cell proliferation assay. Compounds 17a and 17b exhibited potent anti-cell proliferation activity with IC50values in the range of ～3.0?μM and ～0.1–0.6?μM, respectively against these cell lines. Preliminary mechanism of action studies indicates that these compounds initiate caspase dependent apoptosis. Also, compounds 16d, 16f, 17a and 17d exhibited excellent anti-inflammatory activity comparable to well-known NSAID indomethacin and better to bacillamide, when evaluated using carrageenan induced rat hind paw oedema method.

Ethyl 2-((4-Chlorophenyl)amino)thiazole-4-carboxylate and Derivatives Are Potent Inducers of Oct3/4

The octamer-binding transcription factor 4 (Oct3/4) is a master gene in the transcriptional regulatory network of pluripotent cells. Repression of Oct3/4 in embryonic stem cells (ESCs) is associated with cell differentiation and loss of pluripotency, wher