97188-28-8Relevant articles and documents
A red-light-activated sulfonamide porphycene for highly efficient photodynamic therapy against hypoxic tumor
Cheng, Xiao-Lan,Deng, Guowei,Fan, Jiaojiao,Han, Tao,Hau, Sam Chun-Kit,Kwong, Daniel W. J.,Li, Defang,Li, Minjing,Liu, Xiaona,Lu, Jun,Mak, Nai-Ki,Pan, Zhaohai,Qin, Yao,Shiu, Kwok Keung,Wang, Yuzhi,Yan, Ting,Zhang, Kai,Zhang, Xin,Zheng, Qiusheng
, (2020/10/06)
Photodynamic therapy (PDT) is an emerging alternative cancer treatment modality that utilizes photo-sensitivity to cause cell death upon photo-irradiation. However, PDT efficiency has been hampered by tumor hypoxia, blue-shifted excitation wavelengths, an
Synthesis and evaluation of various heteroaromatic benzamides as analogues of –ylidene-benzamide cannabinoid type 2 receptor agonists
Moir, Michael,Boyd, Rochelle,Gunosewoyo, Hendra,Montgomery, Andrew P.,Connor, Mark,Kassiou, Michael
supporting information, (2019/08/12)
The CB2 receptor is an attractive target for the treatment of a wide range of diseases and pathological conditions. Compounds that selectively activate the CB2 receptor are desirable as this avoids CB1-mediated psychoactive effects. Heteroarylidene-benzamides have demonstrated efficacy as selective CB2 receptor agonists. We aimed to expand the structure-activity relationship studies of this series of compounds by investigating the heteroaromatic core via the synthesis and in vitro evaluation of a small library of various heteroaromatic benzamide analogues. As heteroaromatic amides are privileged scaffolds in drug design, methods to synthesise them are of interest. Concise and reliable synthetic strategies were developed to access these novel analogues. The –ylidene-benzamide moiety is shown to be essential for CB activity as all amide derivatives exhibit no functional activity at either CB2 or CB1 receptors.
Pyrrole chemistry. XXVIII. Substitution reactions of 1-(phenylsulfonyl)pyrrole and some derivatives
Anderson, Hugh J.,Loader, Charles E.,Xu, Ru Xun,Le, Nghia,Gogan, Niall J.,et al.
, p. 896 - 902 (2007/10/02)
The preparative value of the 1-(phenylsulfonyl) N-blocking and directing group for the synthesis of 3-acylpyrroles has been further evaluated.Acetylation and benzoylation are strongly regiospecific and give good yields.However, the regiospecificity is not general and other substitution reactions give mixtures of 2- and 3-substitution or even mostly 2-substitution.Friedel and Crafts tert-butylation gives 3-tert-butyl-1-(phenylsulfonyl)pyrrole and provides a useful route to tert-butylpyrrole, but ethylation and isopropylation give mixtures.Acylations of 2- and 3-alkyl-1-(phenylsulfonyl)pyrroles show little evidence of useful regiospecificity.