Discovery of SIPI6473, a New, Potent, and Orally Bioavailable Multikinase Inhibitor for the Treatment of Non-small Cell Lung Cancer

Gu, Xiu; Zhang, Zi-Xue; Jiao, Min-Ru; Peng, Xin-Yan; Li, Jian-Qi; Zhang, Qing-Wei

According to the binding model of Erlotinib with EGFR protein, compound B5 (also named SIPI6473) was designed by conformational restriction. B5 inhibited the activity of several kinases (such as EGFR, VEGFR2, and PDGFRα) that contributed to NSCLC development. In vivo study also showed that B5 inhibited tumor growth without signs of adverse effects in the A549 xenograft model. B5 may represent a new and promising drug for the treatment of NSCLC. EGFR, epidermal growth factor receptor; NSCLC, non-small cell lung cancer.

Phenolic Constituents from the Stems of Morus nigra and their α-Glucosidase Inhibitory Activities

Wang, Ling-Ling; Xu, Liang-Jin; Ma, Meng-Jie; Huang, Chun-Yue; Wu, Tong; Hu, Xiao

A new sanggenon-type flavanone, nigragenon F (1), together with 11 known compounds, were isolated from the stems of Morus nigra. α-glucosidase inhibitory effect test provided different structure-type α-glucosidase inhibitors from M. nigra, not only enriching the library of natural α-glucosidase inhibitors, but also laying experimental basis for the development and utilization of M. nigra as hypoglycemic medicinal plant resources.

Synthesis and Antitumor Activity of (3-Hydroxyacrylato-O,O′) Diammineplatinum(II)

Shu, Yong-Zhi; Lin, Jun; Zhu, Bao-Quan; Liu, Quan-Hai; Zhou, Bin; Hu, Hai-Feng; Ju, Dian-Wen

This paper firstly synthetized two platinum(II) complexes with Michael acceptor 3-hydroxyacrylic acid as the leaving group. Results from MTT assay showed that the anticancer effects of complexes 1 and 2 were similar to that of oxaliplatin in two human cancer cell lines (HCT-116 and A549). An in vivo study showed that administration of complexes 1 at a higher dose and a longer interval may serve as promising drug candidates in cancer therapy.

Synthesis of Natural Product-Like Tricyclic Higher-Carbon Sugar Nucleosides

Yuan, Xiao-Han; Wang, Shuai; Wang, Xiao-Ning; Yu, Bin; Liu, Hong-Min

A series of structurally novel bis-uracil containing tricyclic higher-carbon sugar nucleosides (4a-e) were firstly synthesized using D-xylose as the starting material and the classical Vorbruggen glycosylation as the key synthetic step. The synthetic routes are straightforward, high-yielding, and could be utilized for accessing more analogs for biological screens.

Synthesis of a Novel PTH1–34 Analog with Increased Human Serum Albumin Affinity

Ruan, Si-Da; Dong, Yuan-Zhen; Lu, Jian-Guang; Zhao, Meng-Jia; Lu, Wei-Gen; Feng, Jun

This approach provides a novel PTH1-34 analog, PTH-Lys27-AGC, which may be along-acting agent for osteoporosis treatment in the future.

The Expression of Recombinant Human Serum Albumin in the Mammary Gland of Transgenic Mice

Gong, Gui-Hua; Han, Shu; Huang, Xiao-Ling; Xie, Li-Ping; Zhang, Wei; Xu, Lei; Hu, You-Jia

In this study, an HSA minigene, containing the cDNA of HSA and an intron 1, was firstly constructed. A 2 chickenglobin insulator was added upstream of the promoter as a transcriptionenhancer, while a 7.9 kb αs1-casein 3′ flank sequence was used to strengthen the transcription termination located at the downstream of the expression cassette. The strategy of rHSA expression construct provides an alternative of successful expressions of rHSA, and probably other RPs, in the mammary glands of transgenic mice. HSA, human serum albumin, rHSA, recombinant HAS, RPs, recombinant proteins.