32705-79-6Relevant articles and documents
Platinum(II) complexes with R2edda ligands (R = Me, Et, n-Pr; Edda = ethylenediamine-N,N′-diacetate): Synthesis and characterization
Kalucrossed D Signerovi?, Goran N.,Panteli?, Neboj?a,Eichhorn, Thomas,Bette, Martin,Wagner, Christoph,Zmejkovski, Bojana B.,Schmidt, Harry
, p. 53 - 59 (2014)
Three novel complexes of platinum(II) with R2edda bidentate ligands [PtCl2(R2edda)] (R = Me, Et, n-Pr; edda = ethylenediamine-N,N′-diacetate; 1-3), are synthesized and characterized by IR and NMR spectroscopy and elemental analysis. All complexes exist in three stereoisomeric forms (R,R), (S,S) and (R,S)(S,R). In addition crystal structure of one platinum(IV) complex [PtCl4((n-Pr)2edda)], 4, is presented. Furthermore, in order to assign stereoisomers of 1-3, a reduction of racemic [PtCl4(Et2edda)] by ascorbic acid to [PtCl 2(Et2edda)] (2) was performed and analyzed by 1H NMR. Time-depending 1H NMR spectroscopic experiments were implemented to study the stability of ethylenediamine-N,N′-diacetate diesters. Finally, the in vitro cytotoxic activity of complexes 1-3 was studied on 11 tumor cell lines, 518A2 (melanoma), 8505C (human thyroid carcinoma), A253 (head and neck tumor), A431 (cervix), A549 (lung), A2780 (ovarian), MCF-7 (breast) and HT-29, HCT-8, DLD-1, SW1736 (all colon) by the SRB colorimetric assay method. Complex 3 showed the highest action against ovarian (A2780) cells with an IC50 value 51 ± 1 μM.
Dimer ester micromolecule PROTACs for inducing MDM2 to self-degrade E3 ubiquitin ligase
-
Paragraph 0133; 0140; 0141; 0168, (2018/10/19)
The invention provides dimer ester micromolecule PROTACs for inducing MDM2 to self-degrade E3 ubiquitin ligase. The structure of the PROTACs is shown in the specification, wherein in a compound (I), L1 is C1-C30 linear or branched alkyl with or without a substituent group, and any carbon atom in L1 is optionally replaced by heteroatom; R1, R2, R3 and R4 are C1-C30 linear or branched alkyl with orwithout a substituent group, C1-C30 aryl with or a without substituent group, C1-C30 linear or branched alkylaryl with or without a substituent group or C1-C30 linear or branched aryl alkyl with or without a substituent group respectively and independently; X1, X2, X3 and X4 are halogen respectively and independently.
Dimer amide micromolecule PROTACs for inducing MDM2 to self-degrade E3 ubiquitin ligase
-
Paragraph 0132; 0139; 0140, (2018/10/19)
The invention provides dimer amide micromolecule PROTACs for inducing MDM2 to self-degrade E3 ubiquitin ligase. The structure of the PROTACs is shown in the specification, wherein in a compound (I), L1 is C1-C30 linear or branched alkyl with or without a substituent group, and any carbon atom in L1 is optionally replaced by heteroatom; R1, R2, R3 and R4 are C1-C30 linear or branched alkyl with orwithout a substituent group, C1-C30 aryl with or without a substituent group, C1-C30 linear or branched alkylaryl with or without a substituent group or C1-C30 linear or branched aryl alkyl with or without a substituent group respectively and independently; X1, X2, X3 and X4 are halogen respectively and independently.
INHIBITORS OF (ALPHA-V)(BETA-6) INTEGRIN
-
Paragraph 0201; 0202, (2018/09/16)
Disclosed are small molecule inhibitors of αvβ6 integrin, and methods of using them to treat a number of diseases and conditions.
Containing piperazinone quinazoline ketone PARP - 1/2 inhibitor and its preparation method, pharmaceutical composition and use thereof (by machine translation)
-
Paragraph 0291; 0292, (2017/09/08)
The invention discloses a new class of containing piperazinone quinazoline - 2, 4 (1 H, 3 H) - dione PARP - 1/2 inhibitor, and its preparation and pharmaceutical composition and use. Specifically, the invention relates to the general formula I shown containing of the piperazinone quinazoline - 2, 4 (1 H, 3 H) - dione derivatives and their pharmaceutically acceptable salt, and its preparation method, comprising one or more of the compounds of the composition, and the compounds in the preparation, the prevention and/or treatment with PARP - 1/2 of a disease associated with the use of the medicament. (by machine translation)
MACROCYLIC PYRIMIDINE DERIVATIVES
-
Page/Page column 152, (2015/11/02)
The present invention relates to substituted macrocylic pyrimidine derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention have EF2K inhibitory activity and optionally also Vps34 inhibitory activity. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
Introduction of substituents on the 2-oxo-piperazine skeleton by [3+2] cycloaddition and subsequent transformation
Wierschem, Frank,Rück-Braun, Karola
, p. 431 - 436 (2007/10/03)
The 3,4-substituted 2-oxo-piperazines 5-9 are obtained by [3+2] cycloaddition from nitrone 1 and a variety of alkenes. Subsequent functionalization of the bicyclic adducts involves reductive N-O bond cleavage. A route towards libraries of immobilized 1,3-aminoalcohols with a 3,4-substituted 2-oxo-piperazine scaffold is briefly discussed for adducts derived from N-substituted maleic imides.