- Fluorine-substituted bimolecular carbazole derivative as well as preparation method and application thereof
-
The invention discloses a fluorine-substituted bimolecular carbazole derivative represented by a formula (I) or pharmaceutically acceptable salt thereof. R1, R2, R3, R4 and R5 are defined in the specification. The fluorine-substituted bimolecular carbazole derivative or the pharmaceutically acceptable salt thereof provided by the invention can be used for preparing a DNA methyltransferase inhibitor or a histone demethylase inhibitor, and in-vitro cancer cell anti-proliferation tests prove that the fluorine-substituted bimolecular carbazole derivative has anti-proliferation activity on cancer cells.
- -
-
Paragraph 0098-0099; 0108-0109
(2020/07/08)
-
- Fluorine-substituted monocarbazole derivative as well as preparation method and application thereof (by machine translation)
-
The invention belongs to the field of pharmaceutical chemistry, and relates to a fluorine-substituted monocarbazole derivative which is one or more of compounds represented by formula (I) and formula (II) or a pharmaceutically acceptable soluble salt formed by a compound represented by formula (II). The fluorine-substituted monocarbazole derivatives obtained in the application can be used for preparing DNA methyltransferase inhibitors or histone demethylase inhibitors. The fluorine-substituted monocarbazole derivative has an inhibitory effect on the proliferation of cancer cells and can be used for preparing medicaments for treating and/or preventing cancer. An in-vitro cancer cell proliferation inhibition test shows that the fluorine-substituted monocarbazole compound obtained by the invention shows anti-proliferation activity against human lung cancer cells (A549), human colon cancer cells (HCTCTCT116), human gastric cancer cells (MNK NK NK-45), human liver cancer cells (HepepepG2), RPMI PMI PMI PMI PMI PMI and Karpppp289. (by machine translation)
- -
-
Paragraph 0206-0210
(2020/06/20)
-
- Enantiomerically pure 2-piperazinemethanols as novel chiral ligands of oxazaborolidine catalysts in enantioselective borane reductions
-
Novel enantiomerically pure 2-piperazinemethanols (3-5) were synthesized from 2-piperazinecarboxylic acid 1. The asymmetric reduction of aromatic ketones, ketimine and oxime ether has been performed with reagents prepared from 2-piprazinemethanol and borane to yield enantiomerically enriched alcohols and amines, respectively. The preferred absolute configuration of the product was dependent on the structure of the sulfonyl substituent in the chiral ligand.
- Inoue, Tsutomu,Sato, Daisuke,Komura, Kenichi,Itsuno, Shinichi
-
p. 5379 - 5382
(2007/10/03)
-
- A potent new class of κ-receptor agonist: 4-Substituted 1-(arylacetyl)- 2-[(dialkylamino)methyl]piperazines
-
The synthesis of 4-substituted 1-(arylacetyl)-2- [(alkylamino)methyl]piperazines (10-22, 26, 27, and 30-33) and their activities as κ-opioid receptor agonists are described. This includes a range of 4-acyl and 4-carboalkoxy derivatives with the latter ser
- Naylor,Judd,Lloyd,Scopes,Hayes,Birch
-
p. 2075 - 2083
(2007/10/02)
-