130895-82-8Relevant academic research and scientific papers
Total synthesis and application of natural product of 7-hydroxy novel lamellarin A and analogues of natural product of 7-hydroxy novel lamellarin A
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Paragraph 0120-0122, (2019/11/12)
The invention belongs to the technical field of pharmaceutical and chemical engineering, and provides total synthesis and application of a natural product of 7-hydroxy novel lamellarin A and analoguesof the natural product of the 7-hydroxy novel lamellarin A. The invention provides the 7-hydroxy novel lamellarin A natural product and the series of analogues of the 7-hydroxy novel lamellarin A natural product. Tested compounds all have medium to good HIF-1 inhibitory activity, and have no market toxicity under the effective inhibition concentration of HIF-1 of the tested compounds, and it is indicated that the compounds have the potential for treating cancers by inhibiting transcription activating of the HIF-1.
Structure-activity relationships study of neolamellarin A and its analogues as hypoxia inducible factor-1 (HIF-1) inhibitors
Li, Guangzhe,Dong, Huijuan,Ma, Yao,Shao, Kun,Li, Yueqing,Wu, Xiaodan,Wang, Shisheng,Shao,Zhao, Weijie
supporting information, p. 2327 - 2331 (2019/07/09)
The novel marine pyrrole alkaloid neolamellarin A derived from sponge has been shown to inhibit hypoxia-induced HIF-1 activity. In this work, we designed and synthesized neolamellarin A and its series of derivatives by a convergent synthetic strategy. The HIF-1 inhibitory activity and cytotoxicity of these compounds were evaluated in Hela cells by dual-luciferase reporter gene assay and MTT assay, respectively. The results showed that neolamellarin A 1 (IC50 = 10.8 ± 1.0 μM) and derivative 2b (IC50 = 11.9 ± 3.6 μM) had the best HIF-1 inhibitory activity and low cytotoxicity. Our SAR research focused on the effects of key regions aliphatic carbon chain length, aromatic ring substituents and C-7 substituent on biological activity, providing a basis for the subsequent research on the development of novel pyrrole alkaloids as HIF-1 inhibitors and design of small molecule probes for target protein identification.
1,3,4-Thiadiazole Compounds and Their Use in Treating Cancer
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Paragraph 0231-0232, (2017/06/23)
A compound of Formula (I): or a pharmaceutically acceptable salt thereof, where: Q can be 5-methylpyridazin-3-yl, 5-chloropyridazin-3-yl, 6-methylpyridazin-3-yl, or 6-fluoropyridazin-3-yl; R can be hydrogen, fluoro, or methoxy; R1 can be hydrogen, methoxy, difluoromethoxy, or trifluoromethoxy; and R2 can be methyl or ethyl. The compound of formula (I) can inhibit glutaminase, e.g., GLS1.
Enantiomerically pure α-methoxyaryl acetaldehydes as versatile precursors: a facile chemo-enzymatic methodology for their preparation
Singh, Buddh,Gupta, Pankaj,Chaubey, Asha,Parshad, Rajinder,Sharma, Shiromani,Taneja, Subhash C.
experimental part, p. 2579 - 2588 (2009/04/05)
A facile and efficient synthesis of optically active α-methoxyaryl acetic acids (up to 95% ee), α-methoxyaryl ethanols (up to 93% ee) and α-methoxyaryl acetonitriles (up to 93% ee) was achieved via Arthrobacter sp. lipase-catalyzed kinetic resolution of masked aldehydes as the key synthons, that is, α-hydroxyaryl acetaldehyde acetals.
