Li, Guangzhe; Shao, Yujie; Pan, Yue; Li, Yueqing; Wang, Yang; Wang, Liu; Wang, Xu; Shao, Kun; Wang, Shisheng; Liu, Naixuan; Zhang, Jingdong; Zhao, Weijie; Nakamura, Hiroyuki published the artcile< Total synthesis and biological evaluation of 7-hydroxyneolamellarin A as hypoxia-inducible factor-1α inhibitor for cancer therapy>, Application of C6H12ClNO4, the main research area is hydroxyneolamellarin antitumor agent HIF alpha inhibitor; 7-Hydroxyneolamellarin A; Anti-tumor; HIF-1α inhibition; Total synthesis.
7-Hydroxyneolamellarin A (7-OH-Neo A, 1), a natural marine product derived from sponge Dendrilla nigra, was first synthesized with 10% overall yield under the instruction of convergent synthetic strategy. We found that 7-Hydroxyneolamellarin A could attenuate the accumulation of hypoxia-inducible factor-1α (HIF-1α) protein and inhibit vascular epidermal growth factor (VEGF) transcriptional activity, showing well inhibitory effect on HIF-1 signaling pathway. Meantime, 7-Hydroxyneolamellarin A had the well anti-tumor activities, such as inhibiting tumor angiogenesis, proliferation, migration and invasion. More importantly, 7-Hydroxyneolamellarin A exhibited profound anti-tumor effect in mice breast cancer model by suppressing the accumulation of HIF-1α in tumor tissue. Mechanism study demonstrated that 7-Hydroxyneolamellarin A might target the protein with the ability of stabilizing HIF-1α in hypoxia. Due to the excellent water solubility, superior anti-tumor activity and good biocompatibility, 7-OH-Neo A shows the promising potential for being exploited as an anti-tumor agent in near future.
Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 39987-25-2 belongs to class esters-buliding-blocks, and the molecular formula is C6H12ClNO4, Application of C6H12ClNO4.
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Ester – an overview | ScienceDirect Topics