Kryshchyshyn-Dylevych, Anna Radko, Lidia Finiuk, Nataliya Garazd, Myroslav Kashchak, Nataliya Posyniak, Andrzej Niemczuk, Krzysztof Stoika, Rostyslav Lesyk, Roman
Published in
Bioorganic & medicinal chemistry
A series of novel indole-azolidinone hybrids has been synthesized via Knoevenagel reaction of 5-fluoro-3-formyl-1H-indole-2-carboxylic acid methyl ester and some azolidinones differing in heteroatoms in positions 1, 2 and 4. Their anticancer activity in vitro was screened towards MCF-7 (breast cancer), HCT116 (colon cancer), HepG2 (hepatoma), HeLa ...
Lee, Szu Wang, Shih-Wei Yu, Chen-Lin Tai, Huai-Ching Yen, Juei-Yu Tuan, Yu-Lien Wang, Hsueh-Hsiao Liu, Yi-Ting Chen, Shiou-Sheng Lee, Hsueh-Yun
...
Published in
Bioorganic & medicinal chemistry
A series of phenylurea hydroxamic acids incorporating pharmacophores of inhibitors of HDAC inhibitors and VEGFR-2 has been designed. Most of the compounds show antiproliferative activity comparable to that of Vorinostat and Sorafenib, and better EPC inhibitory activity. Enzymatic assays and Western blotting results indicated that compound 14 not on...
Garai, Sumanta Schaffer, Peter C Laprairie, Robert B Janero, David R Pertwee, Roger G Straiker, Alex Thakur, Ganesh A
Published in
Bioorganic & medicinal chemistry
Allosteric modulators of cannabinoid 1 receptor (CB1R) show translational promise over orthosteric ligands due to their potential to elicit therapeutic benefit without cannabimimetic side effects. The prototypic 2-phenylindole CB1R allosteric modulator, GAT211 (1), demonstrates preclinical efficacy in various disease models. The limited systematic ...
Guilinger, John P Archna, Archna Augustin, Martin Bergmann, Andreas Centrella, Paolo A Clark, Matthew A Cuozzo, John W Däther, Maike Guié, Marie-Aude Habeshian, Sevan
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Bioorganic & medicinal chemistry
Libraries of DNA-Encoded small molecules created using combinatorial chemistry and synthetic oligonucleotides are being applied to drug discovery projects across the pharmaceutical industry. The majority of reported projects describe the discovery of reversible, i.e. non-covalent, target modulators. We synthesized multiple DNA-encoded chemical libr...
Luong, Phuong Dube, Danielle H
Published in
Bioorganic & medicinal chemistry
The bacterial glycocalyx is a quintessential drug target comprised of structurally distinct glycans. Bacterial glycans bear unusual monosaccharide building blocks whose proper construction is critical for bacterial fitness, survival, and colonization in the human host. Despite their appeal as therapeutic targets, bacterial glycans are difficult to ...
van der Wildt, Berend Nezam, Madina Kooijman, Esther J M Reyes, Samantha T Shen, Bin Windhorst, Albert D Chin, Frederick T
Published in
Bioorganic & medicinal chemistry
Pharmacological targeting of tumor associated macrophages and microglia in the tumor microenvironment is a novel therapeutic strategy in the treatment of glioblastoma multiforme. As such, the colony stimulating factor-1 receptor (CSF-1R) has been identified as a druggable target. However, no validated companion diagnostic marker for these therapies...
Romanucci, Valeria Giordano, Maddalena Pagano, Rita Agarwal, Chapla Agarwal, Rajesh Zarrelli, Armando Di Fabio, Giovanni
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Bioorganic & medicinal chemistry
Curcumin is a bioactive natural compound with a wide range of pharmacological properties, including antitumor activity; however, its clinical application has been limited because of its low solubility, stability, and bioavailability. In this study, a solid phase approach was proposed for the combinatorial synthesis of a mini library of the mimics o...
Shirey, Ryan J Hart, Jonathan R Sridharan, BanuPriya Novick, Scott J Turner, Lewis D Zhou, Bin Nielsen, Alexander L Eubanks, Lisa M Ueno, Lynn Hixon, Mark S
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Bioorganic & medicinal chemistry
We report the discovery of a fluorescent small molecule probe. This probe exhibits an emission increase in the presence of the oncoprotein MYC that can be attenuated by a competing inhibitor. Hydrogen-deuterium exchange mass spectrometry analysis, rationalized by induced-fit docking, suggests it binds to the "coiled-coil" region of the leucine zipp...
Fujiki, Katsumasa Tanaka, Katsunori
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Bioorganic & medicinal chemistry
An amino group at side chain of lysine residue can be targeted for protein modification because of the convenience for covalent bond formation. We have achieved an efficient protein modification by utilizing amine-clickable 6π-azaelectrocyclization, termed RIKEN click reaction recently, which enabled direct click labeling of protein without any int...
Fu, Zhipeng Zhang, Tao Zhou, Zhongxia Kang, Dongwei Sun, Lin Gao, Shenghua Cherukupalli, Srinivasulu De Clercq, Erik Pannecouque, Christophe Liu, Xinyong
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Bioorganic & medicinal chemistry
To further explore the chemical space surrounding the "hydrophobic channel" of the NNRTI binding pocket (NNIBP), a new series of diarylpyrimidines (DAPYs) were designed and synthesized as potent HIV-1 non-nucleoside RT inhibitors (NNRTIs). The target compounds were evaluated for anti-HIV potency in MT-4 cells. Most of the synthesized DAPYs exhibite...
