77664-95-0Relevant academic research and scientific papers
Synthesis and Resolution of Substituted [5]Carbohelicenes
Usui, Kazuteru,Yamamoto, Kosuke,Shimizu, Takashi,Okazumi, Mieko,Mei, Biao,Demizu, Yosuke,Kurihara, Masaaki,Suemune, Hiroshi
, p. 6502 - 6508 (2015)
Three types of racemic [5]helicenyl acetates (1a, 2, and 3a) were synthesized. The synthesis of 2 was achieved by regioselective oxidation using o-iodoxybenzoic acid. The enzymatic kinetic resolution of 1a-3a was studied. The conversion with the highest rate and ee was obtained using 1a as the substrate and lipase Amano PS-IM as the enzyme. The two enantiomers of 1-[5]helicenol 3b were separated using (1S)-10-camphorsulfonyl chloride as the chiral resolving agent.
A DOR receptor antagonist compound as
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Paragraph 0418; 0419; 0420, (2017/08/19)
The invention provides a compound used as a DOR receptor antagonist. The structural formula of the compound is as shown in the specification. In comparison with the prior art, the invention expounds a pharmaceutical composition and a preparation containin
Efficient Enantioselective Synthesis of Oxahelicenes Using Redox/Acid Cooperative Catalysts
Sako, Makoto,Takeuchi, Yoshiki,Tsujihara, Tetsuya,Kodera, Junpei,Kawano, Tomikazu,Takizawa, Shinobu,Sasai, Hiroaki
supporting information, p. 11481 - 11484 (2016/10/06)
An efficient and enantioselective synthesis of oxa[9]helicenes has been established via vanadium(V)-catalyzed oxidative coupling/intramolecular cyclization of polycyclic phenols. A newly developed vanadium complex cooperatively functions as both a redox and Lewis acid catalyst to promote the present sequential reaction and afford oxa[9]helicenes in good yields with up to 94% ee.
Synthesis and biological evaluation of guanylhydrazone coactivator binding inhibitors for the estrogen receptor
LaFrate, Andrew L.,Gunther, Jillian R.,Carlson, Kathryn E.,Katzenellenbogen, John A.
experimental part, p. 10075 - 10084 (2009/04/06)
Most patients with hormone-responsive breast cancer eventually develop resistance to traditional antiestrogens such as tamoxifen, and this has become a major obstacle in their treatment. We prepared and characterized the activity of a series of 16 guanylhydrazone small molecules that are designed to block estrogen receptor (ER) activity through a non-traditional mechanism, by directly interfering with coactivator binding to agonist-liganded ER. The inhibitory activity of these compounds was determined in cell-based transcription assays using ER-responsive reporter gene and mammalian two-hybrid assays. Several of the compounds gave IC50 values in the low micromolar range. Two secondary assays were used to confirm that these compounds were acting through the proposed non-traditional mode of estrogen inhibitory action and not as conventional antagonists at the ligand binding site.
SUBSTITUTED THIOPHENE CARBOXAMIDE COMPOUNDS FOR THE TREATMENT OF INFLAMMATION
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Page 23, (2010/11/30)
The present invention provides substituted thiophene carboxamide compounds having structural Formula I and isomers, tautomers, polymorphs, carriers, prodrugs, and pharmaceutically acceptable salts thereof, compositions comprising such, and methods for treating diseases associated with kinase activity. More specifically, the present invention provides methods of treatment of a variety of diseases associated with IKK2 including the treatment of inflammation, other inflammation-associated disorders, such as, as an analgesic in the treatment of pain and headaches, arthritis, including but not limited to rheumatoid arthritis, asthma, gastrointestinal conditions such as inflammatory bowel disease, vascular diseases, viral infections such as AIDS, and cancer.
Synthesis of a series of diaminobenzo[f]- and diaminobenzo[h]pyrimido[4,5-b]quinolines as 5-daza tetracyclic nonclassical antifolates
Donkor,Devraj,Queener,Barrows,Gangjee
, p. 1653 - 1661 (2007/10/03)
A series of diaminobenzo[f]- and diaminobenzo[h]pyrimido[4,5-b]quinolines 1-11 were designed as 5-deaza tetracyclic nonclassical, lipophilic antifolates. The compounds were designed as conformationally semi-rigid and rigid analogs of 2,4-diamino-6-phenyl- 12 and 2,4-diamino-7-phenylpyrido[2,3-d]pyrimidines 13 and 14. The target compounds were synthesized by cyclocondensation of chlorovinyl aldehydes obtained from appropriately substituted 1- or 2-tetralone, with 2,4,6-triaminopyrimidine. Compounds 1-11 were evaluated as inhibitors of P. carinii and T. gondii dihydrofolate reductases. These pathogens cause fatal opportunistic infections in AIDS patients. In addition, the selectivity of these agents was evaluated using rat liver dihydrofolate reductase as the mammalian source. In general the benzo[f]pyrimido[4,5-b]quinolines 1-5 were more potent than the corresponding benzo[h]pyrimido[4,5-b]quinoline analogues 6-11 against P. carinii and rat liver dihydrofolate reductase and were equipotent against T. gondii dihydrofolate reductase. Compounds 6-11 were moderately selective towards T. gondii dihydrofolate reductase with IC50s in the 10-7 M range. In contrast analogues 1-5 lacked selectivity against P. carinii or T. gondii dihydrofolate reductase and were, in general, potent inhibitors of rat liver dihydrofolate reductase with IC50s in the 10-8 M range. Analogues 1 and 4 were evaluated against a series of tumor cell lines in vitro and were found to have moderate antitumor activity (IC50 10-6 M). The structure activity/selectivity relationships suggest that benzo[f]pyrimido analogues 1-5 with the phenyl ring substitution in the 'upper' portion of the tetracyclic ring are better accommodated within the rat liver (mammalian) dihydrofolate reductase and P. carinii dihydrofolate reductase active sites compared to the benzo[h]pyrimido analogues 6-11 which have the phenyl ring substitution in the 'lower' portion of the tetracyclic ring. In contrast P. gondii dihydrofolate reductase does not discriminate between the isomers and binds to both series of compounds with similar affinities.
