52814-86-5Relevant academic research and scientific papers
Benzofuran liquid crystal compound and composition thereof
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, (2018/04/01)
The invention discloses a benzofuran liquid crystal compound containing a benzofuran ring. The structural general formula of the liquid crystal compound is (shown in the description), wherein R represents either one of the straight-chain paraffin with the
Design and synthesis of 2-phenylnaphthalenoids and 2-phenylbenzofuranoids as DNA topoisomerase inhibitors and antitumor agents
Hao, Huilin,Chen, Wang,Zhu, Jing,Lu, Chunhua,Shen, Yuemao
, p. 277 - 287 (2015/09/01)
Abstract Eight 2-phenylnaphthalenoids (2PNs) (3a-h) and twenty four 2-phenylbenzofuranoids (2PBFs) (4a - 4j, 5a-5j, 6a, 6f-6h) were successfully designed, synthesized and their antiproliferative and in vitro DNA topoisomerase inhibitory activities were evaluated. Nine compounds (four 2PNs and five 2PBFs) showed either TopoI or TopoIIα inhibitory activities. Six compounds (four 2PNs and two 2PBFs) exhibited potent cytotoxicity with IC50 values for 72 h exposure ranging from 0.3 to above 20 μM against MDA-MB-231, MDA-MB-435, HepG2 and PC3 cell lines. The two 2PBFs displayed comparable and even better antiproliferative as well as TopoIIα inhibitory activities than 2PNs. Interestingly, the active 2PBFs displayed different mechanisms of TopoIIα inhibition from that of 2PNs, suggesting that the chromophore scaffold replacement may result in a change of the binding site of inhibitors to TopoIIα. Furthermore, the mechanisms of antiproliferation on MDA-MB-231 cells indicate that compounds 5a and 5f are promising for further development of anticancer agents. The results of this study reveal that the evolutionary strategy of medicinal chemistry through scaffold hopping is a promising strategy for structure optimization of TopoIIα inhibitors.
PHARMACEUTICAL COMPOSITIONS AND METHODS OF PREVENTING, TREATING, OR INHIBITING INFLAMMATORY DISEASES, DISORDERS, OR CONDITIONS OF THE SKIN, AND DISEASES, DISORDERS, OR CONDITIONS ASSOCIATED WITH COLLAGEN DEPLETION
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, (2009/01/23)
The present invention provides compositions and methods for preventing, treating, or inhibiting inflammatory diseases, disorders, or conditions of the skin, and diseases, disorders, or conditions associated with collagen depletion using one or more estrogenic agents.
Substituted 2-phenyl benzofurans as estrogenic agents
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, (2008/06/13)
This invention provides estrogen receptor modulators of formula I, having the structure wherein R, R′, A, A′, X, Y, and Y are as defined in the specification, or a pharmaceutically acceptable salt thereof.
An expeditious synthesis of polyhydroxylated 2-arylbenzo[b]furans
Dupont, Romain,Cotelle, Philippe
, p. 5585 - 5589 (2007/10/03)
An expeditious synthesis of polyhydroxylated 2-arylbenzo[b]furans is described. The key steps are the conversion of the corresponding polymethoxylated stilbenes into diarylethanoid molecules (epoxide or alcohol) that were demethylated and cyclised using boron tribromide to give the target polyhydroxylated 2-arylbenzo[b]furans.
2-phenylbenzo[B]furans, process for their manufacture and pharmaceutical preparations containing them
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, (2008/06/13)
The invention relates to new furans and thiophenes with the general Formula 1, STR1 in which R1 and R2 independently of one another denote a hydrogen atom, an alkyl group having 1 to 10 carbon atoms, a benzyl group, a group C(O)R4, where R4 is an alkyl or alkoxy group having 1 to 10 carbon atoms or a phenyl radical, or a carbamoyl group --C(O)NR5 R6, where R5 and R6 independently of one another are a hydrogen atom or an alkyl group having 1 to 10 carbon atoms, and n denotes an integer from 0 to 12 if R3 is a hydrogen atom, or n denotes an integer from 4 to 12 if R3 is an amino group --NR7 R8, where R7 and R8 independently of one another represent a hydrogen atom or an alkyl group having 1 to 10 carbon atoms or R7 and R8 together represent an alkylene group --(CH2)m -- or the group --(CH2)2 -- or R3 denotes an amide group --C(O)NR7 R 8, where R7 and R8 have the abovementioned meanings, or R3 denotes a sulphinyl group --S(O)R3, where R9 is the radical --(CH2)m (CF2)o CF3 and m and o are 2, 3, 4, 5 or 6 and x denotes an oxygen or sulphur atom. These new compounds are strong and selective anti-oestrogens, and have therapeutic applications in the treatment of oestrogen-related illnesses.
