101255-84-9Relevant articles and documents
Compound and applications of compound in preparation of anti-hepatitis C virus drugs
-
Paragraph 0398; 0399; 0400, (2017/08/31)
The present invention discloses a compound and applications of the compound in preparation of anti-hepatitis C virus drugs, wherein the structure formula of the compound is represented by a formula I or II, and the compound represented by the formula I or compound represented by the formula II can be subjected to drug combination with other anti-virus drugs such as interferon (PEG IFN-[alpha]), ribavirin (RBV), boceprevir, telaprevir, simeprevir, sofosbuvir, daclatasvir and the like t prepare anti-HCV products and other anti-virus infection products. According to the present invention, the compound has rich functional group diversity and modificability, and the product is relatively easy to separate and purify; the compounds can well inhibit HCV and other viruses, are obtained through phenotype screening, have different antiviral mechanisms, have extremely novel and innovated structures in the anti-virus field, and are not reported in the prior art; and the compound of the present invention has broad development and application prospect.
Flexible estrogen receptor modulators: Design, synthesis, and antagonistic effects in human MCF-7 breast cancer cells
Meegan,Hughes,Lloyd,Williams,Zisterer
, p. 1072 - 1084 (2007/10/03)
Although many series of estrogen receptor antagonists continue to be produced, the majority are direct structural analogues of existing modulators. To examine the tolerance of the estrogen receptor toward flexible ligands, a series of novel flexible estrogen receptor antagonists were prepared and their antiproliferative effects on human MCF-7 breast tumor cells investigated. Each of these compounds deviated from the traditional triphenylethylene backbone associated with common tamoxifen analogues through the introduction of a flexible methylene (benzylic) spacing group between one of the aryl rings and the ethylene group and through variations in the basic side chain moiety. The compounds prepared, when assayed in conjunction with a tamoxifen standard, demonstrated high potency in antiproliferative assays against an MCF-7 human breast cancer cell line with low cytotoxicity and high binding affinity. A computational study was undertaken to investigate the compounds' potential interactions with specific residues within the human estrogen receptor α ligand-binding domain (ER-LBD), predicting these compounds bind in an antiestrogenic fashion within the ER-LBD and interact with those important residues previously identified in the structures of ER-LBD agonist/antagonist cocrystals. These compounds further illustrate the eclectic nature of the estrogen receptor in terms of ligand flexibility tolerance.