设计,合成并评估了具有各种接头结构的新型芳基取代萘C8连接的吡咯并[2,1– c ] [1,4]苯并二氮杂(PBD)共轭物对一组11人的抗癌活性癌细胞系。所有32个结合物显示出抗癌潜力,它们中的一些显示出特别高的活性(0.01-0.19μ中号)。热变性研究显示了相对于DC-81的有效DNA结合能力。在与细胞周期分布有关的生物学活性测定中,这些PBD结合物诱导G 0 / G 1阶段性停滞,也导致p53和caspase-9蛋白水平升高,随后凋亡的细胞死亡。特别地,一种缀合物是该系列中最有希望的候选物,有可能被单独或与现有抗癌疗法组合进行进一步研究。
An Electrophilic Trifluoromethylthiolation of Silylenol Ethers and <i>β</i>
-Naphthols with Diethylaminosulfur Trifluoride and (Trifluoromethyl)trimethylsilane
作者:Perumal Saravanan、Pazhamalai Anbarasan
DOI:10.1002/adsc.201800366
日期:2018.8.6
efficient and general trifluoromethylthiolation of silylenol ethers and β‐naphthols have been accomplished employing the combination of diethylaminosulfur trifluoride (DAST) and (trifluoromethyl)trimethylsilane (CF3TMS) as source of electrophilic trifluoromethylthio moiety for the synthesis of α‐trifluoromethylthiolated carbonyl compounds and β‐naphthols in good yields. Important features of this method
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
申请人:CHANG Chien-Neng
公开号:US20090010884A1
公开(公告)日:2009-01-08
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.