4138-35-6Relevant articles and documents
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Weinstock,May
, p. 3266 (1940)
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Studying Histone Deacetylase Inhibition and Apoptosis Induction of Psammaplin A Monomers with Modified Thiol Group
Bao, Yu,Xu, Qihao,Wang, Lin,Wei, Yunfei,Hu, Baichun,Wang, Jian,Liu, Dan,Zhao, Linxiang,Jing, Yongkui
, p. 39 - 47 (2021/01/26)
Psammaplin A (PsA) is a bromotyrosine disulfide dimer with histone deacetylase (HDAC) inhibition and acts through reduced monomer PsA-SH. We studied the connection of HDAC inhibition, cell growth inhibition, and apoptosis induction of PsA-SH by modifying the -SH group with deletion (6a) or replacement with hydroxamic acid (10b) or benzamide (12g). PsA-SH inhibits HDAC1/2/3 and 6a loses the HDAC inhibition ability. 10b inhibits HDAC1/2/3/6 while 12g shows selective inhibition of HDAC3. PsA-SH and 10b, but neither 6a nor 12g, induce apoptosis in human leukemia HL-60 cells associated with increased acetylation of Histone H3. PsA-SH and 10b inhibit growth of several solid tumor cell lines in vitro and Lewis lung cancer cell growth in vivo. PsA-SH is a simple scaffold for developing selective HDAC inhibitors and induces apoptosis through inhibiting HDAC1/2.
Manufacturing method for 3-(2-chloropropionylamino)propionic acid alkyl ester
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Paragraph 0024-0028, (2021/01/01)
A process for the preparation 3 - (2- chloropropionylamino) propionic acid alkyl esters. The process of the present invention uses alkylacrylates differently than those using β - alanine as a starting material. 3 - (2-chloropropionylamino) propionic acid alkyl ester, which is an intermediate of a uracil compound useful as a herbicide, can be obtained in high yield and high purity without the need for a step of producing a β-alanine methyl ester hydrochloride.