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Wu Y.,Jilin University | Wu Y.,Sunshine Lake Pharmaceutical Co. | Wang K.,Sunshine Lake Pharmaceutical Co. | Li Z.,Sunshine Lake Pharmaceutical Co. | And 4 more authors.
Tetrahedron Letters | Year: 2014

In this Letter, we described a facile method for constructing fused bicyclic 1-arylpyrazol-5-one ring system. We employed various methylene-containing carboxylic acids as the substrates and proved that the pyrazolone ring closure requires activated methylene group in intermediate II. Accordingly, a series of structurally diversified, fused bicyclic 1-arylpyrazol-5-ones was prepared in moderate to high yields using the requisite substrates. © 2013 Elsevier Ltd. All rights reserved.

Wu Y.-J.,Sunshine Lake Pharmaceutical Co. | Sun M.-M.,Sunshine Lake Pharmaceutical Co. | Xi N.,Sunshine Lake Pharmaceutical Co. | Xi N.,Calitor science LLC
Chinese Journal of New Drugs | Year: 2016

Axl receptor tyrosine kinase belongs to TAM (Tyro3, Axl and Mer) subfamily. When activated by its endogenous ligand Gas 6, Axl regulates key processes such as cell survival, growth, and motility, through several downstream pathways. Axl is aberrantly expressed in multiple hematological and epithelial malignancies, and its overactivation is thought to have contributed to drug resistance in both chemotherapy and targeted therapy. Thus, development of Axl kinase inhibitors constitutes a novel approach to inhibit tumor cell proliferation, diminish metastatic potential, and enhance chemosensitivity. In this review, we highlight current understandings of the therapeutic implication of Axl inhibition and its synergetic effects in resensitizing drug resistance cancer cells. We also discuss several known Axl kinase inhibitors, focusing on their structural influence on kinase selectivity and current development stages. © 2016, Chinese Journal of New Drugs Co. Ltd. All right reserved.

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