96068-42-7Relevant academic research and scientific papers
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.
Synthesis and evaluation of biological activities of bis(Spiropyrazolone)cyclopropanes: A potential application against Leishmaniasis
Barreiro-Costa, Olalla,Morales-Noboa, Gabriela,Rojas-Silva, Patricio,Lara-Barba, Eliana,Santamaría-Aguirre, Javier,Bailón-Moscoso, Natalia,Romero-Benavides, Juan Carlos,Herrera, Ana,Cueva, Cristina,Ron-Garrido, Lenin,Poveda, Ana,Heredia-Moya, Jorge
, (2021/08/30)
This work focuses on the search and development of drugs that may become new alternatives to the commercial drugs currently available for treatment of leishmaniasis. We have designed and synthesized 12 derivatives of bis(spiropyrazolone)cyclopropanes. We
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
Polyethylene glycol-bonded triethylammonium l-prolinate: A new biodegradable amino-acid-based ionic liquid for the one-pot synthesis of bis(pyrazolyl)methanes as DNA binding agents
Kordnezhadian, Reza,Shekouhy, Mohsen,Karimian, Somaye,Tavaf, Zohreh,Malek-Hosseini, Saeed,Shahsavani, Mohammad Bagher,Amirghofran, Zahra,Yousefi, Reza,Khalafi-Nezhad, Ali
, p. 16995 - 17012 (2020/11/02)
Polyethylene glycol-bonded triethylammonium l-prolinate ([PEG-TEA]LP) was prepared as a new, highly efficient, reusable and biodegradable amino-acid-based ionic liquid catalyst using cheap and easily accessible starting materials. The [PEG-TEA]LP chemical
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
Synthesis of a new Ni complex supported on CoFe2O4 and its application as an efficient and green catalyst for the synthesis of bis(pyrazolyl)methane and polyhydroquinoline derivatives
Mohammadi, Masoud,Mousavi, Seyedeh Masoumeh,Tamoradi, Taiebeh
, p. 8289 - 8302 (2020/06/09)
Effective research in green chemistry requires new and applicable synthetic techniques. In this regard, for the first time, a green method is reported for the immobilization of iminodiacetic acid-Ni complex on the surface of CoFe2O4
A simple, rapid and effective protocol for synthesis of bis(pyrazolyl)methanes using nickel–guanidine complex immobilized on MCM-41
Kohzadian, Alireza,Filian, Hossein,Kordrostami, Zahra,Zare, Abdolkarim,Ghorbani-Choghamarani, Arash
, p. 1941 - 1953 (2020/01/11)
Abstract: In this paper, a rapid, easy and very efficient method for the synthesis of bis(pyrazolyl)methanes has been reported in the presence of nickel–guanidine complex immobilized on MCM-41 (MCM-41@Gu@Ni) as a recyclable nanocatalyst. This mesoporous s
Greener and facile synthesis of 4,4′-(arylmethylene)bis(3-methyl-1-phenyl-1H-pyrazol-5-ol)s through a conventional heating procedure
Khaligh, Nader Ghaffari,Mihankhah, Taraneh,Gorjian, Hayedeh,Johan, Mohd Rafie
supporting information, p. 3276 - 3286 (2020/08/05)
A new catalytic application of tetraethylammonium L-prolinate for the facile and cleaner synthesis of 4,4′-(arylmethylene)bis(3-methyl-1-phenyl-1H-pyrazol-5-ol)s is developed. This amino acid-based ionic liquid could be recycled up to five runs, and a neg
Greener and practical synthesis of 4,4′-(arylmethylene)bis(3-methyl-1-phenyl-1H-pyrazol-5-ol)s through a conventional heating and a mechanochemical procedure
Khaligh, Nader Ghaffari,Mihankhah, Taraneh
supporting information, p. 4036 - 4043 (2020/09/12)
A new catalytic application of 4,4′-trimethylenedipiperidine for the efficient synthesis of 4,4′-(arylmethylene)bis(3-methyl-1-phenyl-1H-pyrazol-5-ol)s is developed. According to the principles of green chemistry, the reaction was performed by conventiona
Theoretically and experimentally exploring the corrosion inhibition of N80 steel by pyrazol derivatives in simulated acidizing environment
Singh, Ambrish,Ansari,Quraishi,Kaya, Savas
, (2020/01/11)
Acidizing is the important process used in petroleum industry for oil well stimulation. Here, we are exploring the green synthesis of 4,4’-((4-methoxyphenyl)methylene)bis(3-methyl-1-phenyl-1H-pyrazol-5-ol) (PZ-1) and 4,4’-((4-nitrophenyl)methylene)bis(3-m
