167959-18-4

Upstream product

• 857620-61-2 acetic acid-(2-nitro-4-[2]pyridyl-anilide) 
• 875-51-4 4-Bromo-2-nitroaniline 
• 197958-29-5 pyridin-2-ylboronic acid 
• 17997-47-6 2-tri-n-butylstannylpyridine 
• 88-74-4 2-nitro-aniline 

Downstream Products

• 4394-02-9 2-(4-methoxy-3-nitrophenyl)pyridine 
• 104994-90-3 α-(3-amino-4-methoxyphenyl)pyridine 
• 857628-12-7 2-Amino-4-[2]pyridyl-phenol 
• 159958-44-8 2-(4-hydroxy-3-nitrophenyl)pyridine 
• 471241-03-9 4-[2]pyridyl-o-phenylenediamine 

Relevant academic research and scientific papers

Syntheses and structure-activity relationships of novel, potent, and selective trans-2-[3-oxospiro[isobenzofuran-1(3H),1′-cyclohexan]-4′-yl]benzimidazole NPY Y5 receptor antagonists

Syntheses and structure-activity relationships of a novel class of 2-[3-oxospiro[isobenzofuran-1(3H),1′-cyclohexan]-4′-yl]benzimidazole NPY Y5 receptor antagonists are described. Optimization of the lead compound 2a by incorporating substituents into the 5-position or into both the 5- and 6-positions of the benzimidazole core part led to the identification of 5-(5-methyl-1,2,4-oxadiazol-2-yl)benzimidazole (2r: IC50 = 3.3 nM) and 5-(2-methyltetrazol-5-yl)benzimidazole (2u: IC50 = 5.9 nM), both of which are potent, selective, and orally bioavailable Y5 receptor antagonists. Crown Copyright

Trisbenzimidazoles useful as topoisomerase I inhibitors

The present invention provides anti-neoplastic topoisomerase I inhibitors of the formula: STR1 wherein Ar is (C6 -C12)aryl or (5- to 12-membered) heteroaryl comprising 1-3 N, S or non-peroxide O, wherein N is unsubstituted or is substituted with (C1 -C4)alkyl; X is H, CN, CHO, OH, acetyl, CF3, O(C1 -C4)alkyl, NO2, NH2, halogen or halo-(C1 -C4)alkyl; each Y is individually H, (C1 -C4)alkyl or aralkyl; Y' is H or (C1 -C4)alkyl; n is 0 or 1; and each Z is individually H, (C1 -C4)alkyl, halogen or halo(C1 -C4)alkyl; or a pharmaceutically acceptable salt therein.

Terbenzimidazoles useful as antifungal agents

The present invention provides a method of treatment of fungal infection with an antifungal topoisomerase I inhibitor of the formula: STR1 wherein Ar is (C6 -C12)aryl, a (5- to 12-membered) heteroaryl comprising 1-3 N, S or non-peroxide O, wherein N is unsubstituted or is substituted with H, (C1 -C4)alkyl or benzyl; or benzo; X is H, CN, CHO, OH, acetyl, CF3, O(C1 -C4)alkyl, NO2, NH2, halogen or halo-(C1 -C4)alkyl; each Y is individually H, (C1 -C4)alkyl or aralkyl; Y' is H or (C1 -C4)alkyl; n is 0 or 1; and each Z is individually H, (C1 -C4)alkyl, halogen or halo(C1 -C4)alkyl; or a pharmaceutically acceptable salt thereof.

Synthesis and evaluation of terbenzimidazoles as topoisomerase I inhibitors

The synthesis and pharmacological activity of a series of terbenzimidazoles are described. The ability of these derivatives to induce DNA cleavage in the presence of topoisomerase I was evaluated in vitro. These analogs were also assayed for their cytotoxicity in RPMI 8402 cells and the camptothecin-resistant CPT-K5 cells. In addition the potential for these compounds to serve as substrates for MDR1 was also determined. Several terbenzimidazoles exhibited similar cytotoxicity against variants of human tumor cells that either overexpress MDR1 or are camptothecin-resistant.