Synthesis and Structure–Activity Relationships of Lapacho Analogues. 2. Modification of the Basic Naphtho[2,3-<i>b</i>]furan-4,9-dione, Redox Activation, and Suppression of Human Keratinocyte Hyperproliferation by 8-Hydroxynaphtho[2,3-<i>b</i>]thiophene-4,9-diones
of linearly anellated lapacho quinones, naphtho[2,3-b]furan-4,9-dione (7), was modified in the search for novel agents against keratinocyte hyperproliferation. The synthesis and structure–activity relationships of several heterocycle-fused naphthoquinones as well as a full range of 2- and 7-substituted derivatives of one of these, 8-hydroxynaphtho[2,3-b]thiophene-4,9-dione (8a), are described. Out of
在寻找抗角质形成细胞过度增生的新型药物时,对线性带电lapacho醌naphtho [2,3 - b ] furan-4,9-dione(7)的基本结构进行了修改。几种杂环稠合萘醌的合成及其与结构和活性的关系,以及这些8-羟基萘[2,3 - b ]噻吩-4,9-二酮之一的全范围2和7取代衍生物(描述图8a)。总共71种类似物中,特别是2-thenoyl取代的26l,2-nicotinoyl取代的26m和2-oxadiazole取代的35a与抗银屑病药anthralin相比具有优势。使用HaCaT细胞作为模型评估了它们抑制角质形成细胞过度增殖的潜能,并与相对较低的对角质形成细胞的膜破坏作用相结合,这是通过从细胞质中释放出乳酸脱氢酶活性来确定的。关于作用机理,研究了在分离的酶法测定中通过一电子还原和二电子还原来还原lapacho醌的氧化还原,并在基于角质形成细胞的过度增殖测定中证实了它们产生超氧化物的潜力。
INHIBITORS OF HIV REPLICATION
申请人:STURINO Claudio
公开号:US20100261714A1
公开(公告)日:2010-10-14
Compounds of formula (I):
wherein R
1
, R
2
, A
1
, A
2
, A
3
, A
4
, X and Y are as defined herein, are useful as inhibitors of HIV replication.
Fluorine compound and fluorinating agent comprising the compound
申请人:——
公开号:US20040073065A1
公开(公告)日:2004-04-15
A fluorine compound represented by Formula (1) is provided. The above fluorine compound is effective for introducing a fluorine atom into a compound having an active group such as an oxygen-containing functional group, and it can be used for uses of surface treatment, cleaning and coating. Further, after the fluorination reaction, the above compound is recovered and can be reused as a starting material for producing the above fluorine compound, and it is useful for various fluorination processes.
1
(wherein X represents a nitrogen or phosphorus atom; R
0
, R
1
, and R
2
represent hydrogen, an alkyl group or aryl group which may have a substituent, and they each may be the same or different; and R
0
, R
1
, and R
2
may be combined with each other to form a ring).
An unprecedented methodology for the synthesis of a variety of organic amides through the coupling of wide range of unactivated primary, secondary, and tertiary diversified amides, with different amines is reported. The acid-promoted reaction is proposed to proceed through carbonyl activation and is accompanied by broad substrate scope with high tolerance for functional groups.