599191-73-8Relevant articles and documents
A Facile and Effcient Synthesis of Some New Indazole Schiff Bases through Conventional and Microwave Irradiation Conditions
Liu, Xing-Hai,Min, Li-Jing,Shi, Hai-Bo,Wu, Hong-Ke,Zhang, Pei-Pei
, p. 15 - 19 (2021/08/12)
A series of new indazole Schiff bases was synthesized under conventional and microwave irradiation conditions by the reactions of 4-iodo-1H-indazol-3-amine with various substituted aldehydes. Their chemical structures were characterized by proton nuclear
NOVEL INDAZOLE DERIVATIVES AND PHARMACEUTICAL COMPOSITION FOR PREVENTING, ALLEVIATING OR TREATING CANCER CONTAINING THE SAME
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Paragraph 0222-0223, (2020/12/25)
Disclosed are a compound selected from novel indazole derivatives, pharmaceutically acceptable salts thereof, hydrates thereof and stereoisomers thereof, a method for preparing the compound, and a pharmaceutical composition for preventing, alleviating or treating cancer containing the compound as an active ingredient. The novel indazole derivatives exhibit excellent ABL/DDR1 inhibitory efficacy and anti-proliferative efficacy against cancer cells, specifically blood cancer cells, and inhibitory activity against ABL T315I point mutations, thus being useful for the prevention, alleviation or treatment of cancer, specifically blood cancer, especially chronic myelogenous leukemia.
Discovery of novel anti-angiogenesis agents. Part 11: Development of PROTACs based on active molecules with potency of promoting vascular normalization
Shan, Yuanyuan,Si, Ru,Wang, Jin,Zhang, Qingqing,Li, Jing,Ma, Yuexiang,Zhang, Jie
, (2020/08/05)
Our recent investigation is focused on the discovery of anti-angiogenesis agents. Vascular normalization induced by anti-angiogenic agent appears to be a promising strategy. We have developed novel angiogenesis inhibitors with potency of promoting vascular normalization. Herein, we reported the design, synthesis and preliminary evaluation of proteolysis-targeting chimera (PROTACs) based on the previously developed anti-angiogenesis agents. Two PROTACs exhibited potent VEGFR-2 inhibition and anti-proliferative activity against HUVECs. Moreover, they were capable of reducing protein levels of VEGFR-2 in EA.hy926 cells without significant cytotoxicity against HEK293 cells. The novel PROTACs could be used to normalize the abnormal vessels, resulting in efficient delivery of drugs.