Zhao, Shizhen Li, Xinping Wang, Le Peng, Wenjing Ye, Wenling Li, Weiguo Wang, Yan-Dong Chen, Wei-Dong
Published in
Bioorganic & medicinal chemistry
TGR5 is emerging as an important and promising target for the treatment of diabetes, obesity and other metabolic syndromes. A series of novel 1-benzyl-1H-imidazole-5-carboxamide derivatives was designed, synthesized and evaluated in vitro and in vivo. The most potent compounds 19d and 19e exhibited excellent agonistic activities against hTGR5, whic...
Matada, Basavarajaiah Suliphuldevara Pattanashettar, Raviraj Yernale, Nagesh Gunavanthrao
Published in
Bioorganic & medicinal chemistry
Amongst heterocyclic compounds, quinoline is an advantaged scaffold that appears as a significant assembly motif for the development of new drug entities. Quinoline and its derivatives tested with diverse biological activity constitute an important class of compounds for new drug development. Therefore, many scientific communities have developed th...
Bai, Aiping Bielawski, Jacek Bielawska, Alicja Hannun, Yusuf A
Published in
Bioorganic & medicinal chemistry
B13 is an acid ceramidase (ACDase) inhibitor. The two chiral centers of this aromatic amido alcohol lead to four stereoisomers, yet we have little knowledge about its erythro- enantiomers, (1R, 2S) and (1S, 2R). In this paper, for the first time, the synthesis of two erythro- enantiomers is described, and the compounds are evaluated along with two ...
Yamazaki, Diego A S Rozada, Andrew M F Baréa, Paula Reis, Elaine C Basso, Ernani A Sarragiotto, Maria Helena Seixas, Flávio A V Gauze, Gisele F
Published in
Bioorganic & medicinal chemistry
A novel series of arylcarbamate-N-acylhydrazones derivatives have been designed and synthesized as potential anti-cholinesterase agents. In vitro studies revealed that these compounds demonstrated selective for butyrylcholinesterase (BuChE) with potent inhibitory activity. The compounds 10a-d, 12b and 12d were the most potent BuChE inhibitors with ...
Lawrence, Scott A Blankenship, Ross Brown, Robin Estwick, Selina Ellis, Bernice Thangaraju, Arunkumar Datta-Mannan, Amita
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Bioorganic & medicinal chemistry
The neonatal Fc receptor (FcRn) represents a transport system with the potential to facilitate absorption of biologics across the gastrointestinal barrier. How biologics interact with FcRn to enable their gastrointestinal absorption, and how these interactions might be optimized in a biological therapeutic are not well understood. Thus, we studied ...
Hu, Junbo Zhang, Yanli Tang, Na Lu, Yanju Guo, Peng Huang, Ziming
Published in
Bioorganic & medicinal chemistry
This study describes the synthesis of novel 1,3,5-triazine derivatives as potent inhibitors of cervical cancer. The compounds were initially tested for inhibition of PI3K/mTOR, where they showed significant inhibitory activity. The top-ranking molecule (compound 6 h) was further tested against class I PI3K isoforms, such as PI3Kα, PI3Kβ, PI3Kγ and ...
Qin, Jing Qu, Sifeng Zhu, Kongkai Cheng, Yahong Pan, Ge Jing, Weiqiang Liu, Xigong Sun, Xia Liu, Lei
Published in
Bioorganic & medicinal chemistry
Progesterone receptor (PR) antagonists have been found to be effective for treating certain human cancers. However, the steroidal structure of PR antagonists could bind to other hormone receptors, thus leading to serious side effects. On the other hand, non-steroidal PR antagonists have rarely been evaluated for their anti-cancer efficacy. Therefor...
Pomeislová, Alice Otmar, Miroslav Rubešová, Petra Benýšek, Jakub Matoušová, Marika Mertlíková-Kaiserová, Helena Pohl, Radek Poštová Slavětínská, Lenka Pomeisl, Karel Krečmerová, Marcela
...
Published in
Bioorganic & medicinal chemistry
In analogy to antiviral acyclic nucleoside phosphonates, a series of 5-amino-3-oxo-1,2,4-thiadiazol-3(2H)-ones bearing a 2-phosphonomethoxyethyl (PME) or 3-hydroxy-2-(phosphonomethoxy)propyl (HPMP) group at the position 2 of the heterocyclic moiety has been synthesized. Diisopropyl esters of PME- and HPMP-amines have been converted to the N-substit...
Ren, Yulin Kinghorn, A Douglas
Published in
Bioorganic & medicinal chemistry
Cantharidin is a potent natural protein phosphatase monoterpene anhydride inhibitor secreted by several species of blister beetle, with its demethylated anhydride analogue, (S)-palasonin, occurring as a constituent of the higher plant Butea frondosa. Cantharidin shows both potent protein phosphatase inhibitory and cancer cell cytotoxic activities, ...
Su, Shijun Chen, Mei Li, Qin Wang, Yihui Chen, Shuai Sun, Nan Xie, Chengwei Huai, Ziyou Huang, Yinjiu Xue, Wei
...
Published in
Bioorganic & medicinal chemistry
A series of novel penta-1,4-diene-3-one derivatives containing quinazoline and oxime ether moieties were designed and synthesized. Their anticancer activities were evaluated by MTT assay, the results showed that most compounds exhibited extremely inhibitory effects against hepatoma SMMC-7721 cells. In particular, compounds Q2 and Q8 displayed the m...
