54584-72-4

Upstream product

• 16398-07-5 2-chloro-N-(2-hydroxyphenyl)-5-nitrobenzamide 
• 95-55-6 2-amino-phenol 
• 6361-21-3 2-chloro-5-nitrobenzaldehyde 
• 25784-91-2 2-chloro-5-nitrobenzoylchloride 

Downstream Products

• 54584-65-5 1-acetoxy-3-(2-benzooxazol-2-yl-4-nitro-anilino)-propane 
• 54584-64-4 3-(2-benzooxazol-2-yl-4-nitro-anilino)-propan-1-ol 
• 54584-74-6 2-[2-(4-methyl-piperazin-1-yl)-5-nitro-phenyl]-benzooxazole 
• 54584-73-5 2-(5-nitro-2-pyrrolidin-1-yl-phenyl)-benzooxazole 

Relevant academic research and scientific papers

AROMATIC DIAMINE, AN INTERMEDIATE THEREFOR, A METHOD FOR PRODUCING THE AROMATIC DIAMINE, AND A METHOD FOR PRODUCING THE INTERMEDIATE THEREFOR

A novel asymmetric diamine, diamino-2-(benzothiazole-2-yl)diphenyl ether, derivatives therefor, and an intermediate for the compound such as aminonitro-2-(benzothiazole-2-yl)diphenyl ether, dinitro-2-(benzothiazole-2-yl)diphenyl ether, and derivatives fro

Synthesis and in vitro antibacterial and antifungal activities of benzoxazole derivatives

The in vitro antibacterial and antifungal activities of twenty-nine (29) benzoxazole derivatives were tested against fifteen Gram-positive and sixteen Gram-negative strains. Out of the twenty-nine compounds, eighteen compounds 3-5, 7-9, 11-13, 15-25 showed a broad range of activity against tested Gram-positive microorganisms, whereas rest of the compounds 6, 10, 14 and 26-31 were found to be completely inactive against all the tested strains of Gram-positive bacteria. Five compounds 8, 11-13, and 15 showed activities against Gram-negative strains whereas the rest were devoid of any activity. Twenty-one (21) out of twenty-nine (29) compounds possessed antifungal activity. The structures of the synthetic compounds were confirmed by IR, EIMS and 1HNMR spectral data.

Synthesis and biological evaluation of SANT-2 and analogues as inhibitors of the hedgehog signaling pathway

Hedgehog (Hh) signaling plays an important role in cell signaling of embryonic development and adult tissue homeostasis. In vertebrates, the hh gene encodes three different unique proteins: sonic hedgehog (Shh), desert hedgehog (Dhh) and indian hedgehog (Ihh). Disruption of the Hh signaling pathway leads to severe disorders in the development of vertebrates whereas aberrant activation of the Hh pathway has been associated with several malignancies including Gorlin syndrome (a disorder predisposing to basal cell carcinoma, medulloblastoma and rhabdomyosarcoma), prostate, pancreatic and breast cancers. In vivo evidence suggests the antagonism of excessive Hh signaling provides a route to unique mechanism-based anti-cancer therapies. Recently the small molecule SANT-2 was identified as a potent antagonist of Hh-signaling pathway. Here, we describe the synthesis, SAR studies as well as biological evaluation of SANT-2 and its analogues. Fifteen SANT-2 derivatives were synthesized and analyzed for their interference with the expression of the Hh target gene Gli1 in a reporter gene assay. By comparison of structure and activity important molecular descriptors for Gli inhibition could be identified. Furthermore we identified derivative TC-132 that was slightly more potent than the parent compound SANT-2. Selected compounds were tested for Hh related teratogenic effects in the small teleost model medaka. Albeit Gli expression has indicated a 16-fold higher Hh-inhibiting activity than observed for the plant alkaloid cyclopamine, none of the tested compounds were able to induce the cyclopamine-specific phenotype in the medaka assay.

MEDIATORS OF HEDGEHOG SIGNALING PATHWAYS, COMPOSITIONS AND USES RELATED THERETO

The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist of formula (I) in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity.

Benzoxazole LPAAT-B inhibitors and uses thereof

The invention relates to benzoxazoles and the use thereof to inhibit lysophosphatidic acid acyltransferase β (LPAAT-β) activity. The invention further relates to methods of treating cancer using said benzoxazoles. The invention also relates to methods for screening for LPAAT-β activity.