96068-42-7Relevant articles and documents
Discovery of novel inhibitors of human phosphoglycerate dehydrogenase by activity-directed combinatorial chemical synthesis strategy
Zhou, Xia,Tan, Yuping,Gou, Kun,Tao, Lei,Luo, Yuan,Zhou, Yue,Zuo, Zeping,Sun, Qingxiang,Luo, Youfu,Zhao, Yinglan
, (2021/07/26)
Serine, the source of the one-carbon units essential for de novo purine and deoxythymidine synthesis plays a crucial role in the growth of cancer cells. Phosphoglycerate dehydrogenase (PHGDH) which catalyzes the first, rate-limiting step in de novo serine biosynthesis has become a promising target for the cancer treatment. Here we identified H-G6 as a potential PHGDH inhibitor from the screening of an in-house small molecule library based on the enzymatic assay. We adopted activity-directed combinatorial chemical synthesis strategy to optimize this hit compound. Compound b36 was found to be the noncompetitive and the most promising one with IC50 values of 5.96 ± 0.61 μM against PHGDH. Compound b36 inhibited the proliferation of human breast cancer and ovarian cancer cells, reduced intracellular serine synthesis, damaged DNA synthesis, and induced cell cycle arrest. Collectively, our results suggest that b36 is a novel PHGDH inhibitor, which could be a promising modulator to reprogram the serine synthesis pathway and might be a potential anticancer lead worth further exploration.
In situ decorated Mn–lysine complex on magnetic nanoparticles as a novel and reusable nanocatalyst in the synthesis of 4,4′-(arylmethylene)-bis-(3-methyl-1-phenyl-1H-pyrazol-5-ols) derivatives
Tamoradi, Taiebeh,Mousavi, Seyedeh Masoumeh,Karmakar, Bikash
, p. 2919 - 2929 (2021/05/11)
In this work, we report a new and recoverable catalyst by anchoring the Mn–Lysine complex on the surface of CoFe2O4 magnetic nanoparticles through a simple, rapid and eco-friendly procedure. The successful synthesis of this nanostruc
Pd(0)-guanidine?MCM-41: a very effective catalyst for rapid production of bis (pyrazolyl)methanes
Filian, Hossein,Ghorbani-Choghamarani, Arash,Karami, Amirali,Kohzadian, Alireza,Mohammadi, Masoud
, (2020/03/26)
In this research, a rapid, green and efficient protocol for synthesis of bis (pyrazolyl)methane derivatives in the presence of Pd(0)-guanidine?MCM-41 catalysts under solvent-free conditions by the following two methods has been reported: (i) via the one-p