Li, Zhenyu Wu, Xingkang Jia, Lejiao Li, Jun Zhang, Rui Tang, Hui Li, Zhiying Bu, Huagang Shen, Chengwu
Published in
Bioorganic & medicinal chemistry letters
A series of novel 2-arylbenzimidazoles have been designed, synthesized and evaluated for their inhibitory activity against IDH2 R140Q mutant. The preliminary results indicated that four compounds 7b, 7c, 7m and 7r displayed the potent inhibitory activity against IDH2 R140Q mutant. Among them, compound 7c showed the highest inhibitory activity, with...
Liu, Dandan Cui, Xikai Dhawane, Abasaheb N Chivukula, Vasanta Iyer, Suri S
Published in
Bioorganic & medicinal chemistry letters
Early and accurate diagnosis of influenza viruses can decrease its harmful impact. Here, we have synthesized fluorescent sialic acid derivatives that are cleaved by influenza neuraminidases (NAs) and not by Streptococcus pneumoniae that also inhabits the human olfactory. We have also attempted to develop assays that could differentiate between infl...
Narita, Sho Kobayashi, Naohiro Mori, Kanna Sakurai, Kaori
Published in
Bioorganic & medicinal chemistry letters
Alkyne-labelled proteins are generated as key intermediates in the chemical probe-based approaches to proteomics analysis. Their efficient and selective detection and isolation is an important problem. We designed and synthesized azide-functionalized gold nanoparticles as new clickable capture reagents to streamline click chemistry-mediated capture...
Consalvi, Sara Scarpecci, Cristina Biava, Mariangela Poce, Giovanna
Published in
Bioorganic & medicinal chemistry letters
The biosynthetic pathways of amino acids are attractive targets for drug development against pathogens with an intracellular behavior like M. tuberculosis (Mtb). Indeed, while in the macrophages Mtb has restricted access to amino acids such as tryptophan (Trp). Auxotrophic Mtb strains, with mutations in the Trp biosynthetic pathway, showed reduced ...
Wang, Jiming Zhang, Xiangyu Yan, Jiangkun Li, Wei Jiang, Qinwen Wang, Xinran Zhao, Dongmei Cheng, Maosheng
Published in
Bioorganic & medicinal chemistry letters
Histone lysine-specific demethylase 1 (LSD1) was the first discovered histone demethylase. Inactivating LSD1 or downregulating its expression inhibits cancer-cell development, and thus, it is an attractive molecular target for the development of novel cancer therapeutics. In this study, we worked on the structural optimization of natural products a...
Yang, Yifeng Li, Yingxiu Hou, Yunlei Qin, Mingze Gong, Ping Liu, Ju Zhao, Yanfang
Published in
Bioorganic & medicinal chemistry letters
A series of novel 4-phenoxyquinoline derivatives containing 3-oxo-3,4-dihydro-quinoxaline moiety were synthesized and evaluated for their antiproliferative activity against five human cancer cell lines (A549, H460, HT-29, MKN-45 and U87MG) in vitro. Most of the tested compounds exhibited more potent inhibitory activities than the positive control f...
Wang, Jian-Ta Peng, Jin-Gang Zhang, Ji-Quan Wang, Zhong-Xiao Zhang, Yi Zhou, Xun-Rong Miao, Jing Tang, Lei
Published in
Bioorganic & medicinal chemistry letters
Four series of berberine derivatives were designed and synthesized. All the synthetic compounds were screened for in vitro glucose consumption activity in HepG2 cell lines. The results showed that most of the tested compounds exhibited potent hypoglycemic activity, and the most potent compound 20b exhibited its potency by 3.23-fold of berberine, 1....
Gu, Zheng-Song Wang, Wen-Tao Qian, Hao Zhou, Ai-Nan Sun, Hong-Bin Zhang, Qing-Wei Li, Jian-Qi
Published in
Bioorganic & medicinal chemistry letters
A series of novel aralkyl piperazine and piperidine derivatives were synthesized, and evaluated for their serotonin reuptake inhibitory and 5-HT1A/5-HT7 receptors affinities activity. Antidepressant activities in vivo of the selective compound were screened using the forced swimming test (FST) and tail suspension test (TST). The results indicated t...
Vickery, Christopher R McCulloch, Ian P Sonnenschein, Eva C Beld, Joris Noel, Joseph P Burkart, Michael D
Published in
Bioorganic & medicinal chemistry letters
Modular synthases, such as fatty acid, polyketide, and non-ribosomal peptide synthases (NRPSs), are sophisticated machineries essential in both primary and secondary metabolism. Various techniques have been developed to understand their genetic background and enzymatic abilities. However, uncovering the actual biosynthetic pathways remains challeng...
Li, Yan-Wei Li, Xiang-Yu Li, Shanji Zhao, Li-Min Ma, Juan Piao, Hu-Ri Jiang, Zhe Jin, Cheng Hua Jin, Xuejun
Published in
Bioorganic & medicinal chemistry letters
The transcription factor hypoxia-inducible factor-1α (HIF-1α) plays an important role in apoptosis, metastasis, and proliferation and is recognized as an important potential therapeutic target for cancer. Six series of 3(5)-(6-methylpyridin-2-yl)-4-(quinolin-4-yl)pyrazoles (11a-d, 12a-d, and 18a-d) and 3(5)-(6-methylpyridin-2-yl)-4-(2-phenyl-pyridi...
