99207-32-6Relevant academic research and scientific papers
De-novo designed β-lysine derivatives can both augment and diminish the proliferation rates of E. coli through the action of Elongation Factor P
Connon, Stephen J.,Ghanim, Magda,Kelly, Vincent P.,McDonnell, Ciara M.,Mike Southern, J.
, (2022/01/24)
An investigation into the effect of modified β-lysines on the growth rates of eubacterial cells is reported. It is shown that the effects observed are due to the post translational modification of Elongation Factor P (EFP) with these compounds catalysed b
METHODS FOR DELAYING, PREVENTING, AND TREATING ACQUIRED RESISTANCE TO RAS INHIBITORS
-
Paragraph 00460, (2022/01/04)
The present disclosure relates to compositions and methods for the treatment of diseases or disorders (e.g., cancer) with bi-steric inhibitors of mTOR in combination with RAS inhibitors. Specifically, in some embodiments this disclosure includes compositions and methods for inducing apoptosis of tumor cells and/or for delaying, preventing, or treating acquired resistance to RAS inhibitors using bi-steric mTOR inhibitors.
HETEROBIFUNCTIONAL MOLECULES AS TEAD INHIBITORS
-
Paragraph 0258; 0263-0264, (2021/09/11)
The invention relates to compounds and methods of using said compounds, as well as pharmaceutical compositions containing such compounds, for treating diseases and conditions mediated by TEAD, such as cancer.
Functionalized Polyhydroquinolines from Amino Acids Using a Key One-Pot Cyclization Cascade and Application to the Synthesis of (±)-Δ7-Mesembrenone
Bélanger, Guillaume,Gallagher-Duval, Shawn,Lapointe, Vincent
supporting information, p. 8606 - 8611 (2021/11/17)
Substituted polyhydroquinolines are ubiquitous skeletal cores found in drugs and bioactive natural products. As a new route to access this motif, we successfully developed a one-pot cyclization cascade with high chemocontrol and diastereoselectivity. The sequence generates two cycles, three carbon-carbon bonds, and an all-carbon quaternary center in a highly convergent process. Functionalized polyhydroquinolines and congeners can be accessed from commercially available amino acids. This versatile and robust strategy was applied to the synthesis of (±)-Δ7-mesembrenone.
C26-LINKED RAPAMYCIN ANALOGS AS MTOR INHIBITORS
-
Paragraph 00448, (2019/11/21)
The present disclosure relates to mTOR inhibitors. Specifically, the embodiments are directed to compounds and compositions inhibiting mTOR, methods of treating diseases mediated by mTOR, and methods of synthesizing these compounds.
C40-, C28-, AND C-32-LINKED RAPAMYCIN ANALOGS AS MTOR INHIBITORS
-
Paragraph 00513, (2019/11/19)
The present disclosure relates to mTOR inhibitors. Specifically, the embodiments are directed to compounds and compositions inhibiting mTOR, methods of treating diseases mediated by mTOR, and methods of synthesizing these compounds.
PYRIMIDINE COMPOUNDS USEFUL AS TYROSINE KINASE INHIBITORS
-
Paragraph 141; 154, (2019/07/13)
The present disclosure provides pyrimidine compounds useful as tyrosine kinase inhibitors, and particularly epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2) inhibitors. The disclosed EGFR inhibitors are effective
RAPAMYCIN ANALOGS AS MTOR INHIBITORS
-
Paragraph 00344, (2018/12/03)
The present disclosure relates to rapamycin analogs of the general Formula (I). The compounds are inhibitors of mTOR and thus useful for the treatment of cancer, immune-mediated diseases and age related conditions.
ANTICANCER AGENT DELIVERY MOLECULE
-
, (2017/08/04)
PROBLEM TO BE SOLVED: To provide a compound which can be used as an anticancer agent targeting a cancer cell that highly expresses Lysine-specific demethylase 1 (LSD1) or salt thereof. SOLUTION: The present invention provides a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof, where Ar, R1, R2, L, Z, p, q, *1 and *2 are as defined in the specifications. SELECTED DRAWING: None COPYRIGHT: (C)2017,JPOandINPIT
Development of polyamine transport ligands with improved metabolic stability and selectivity against specific human cancers
Muth, Aaron,Kamel, Joseph,Kaur, Navneet,Shicora, Allyson C.,Ayene, Iraimoudi S.,Gilmour, Susan K.,Phanstiel, Otto
, p. 5819 - 5828 (2013/08/23)
Polyamine homeostasis is critical for life and is accomplished via a balance of polyamine biosynthesis, degradation, and transport. Rapidly dividing cancer cells have been shown to have high polyamine transport activity compared to normal cells, likely due to their high requirement for polyamine metabolites. The polyamine transport system (PTS) is a therapeutically relevant target, as it can provide selective drug delivery to cancer cells. This report describes the synthesis and biological evaluation of multimeric polyamine derivatives as efficient PTS ligands. Arylmethyl-polyamine derivatives were synthesized to address two important concerns in PTS drug design: (a) PTS selectivity and (b) stability to amine oxidases. N1,N1′-[Naphthalene-1, 4-diylbis(methylene)]bis{N4-[4-(methylamino)butyl])butane-1,4- diamine}, 3b, was found to have an optimal balance between these parameters and demonstrated excellent targeting of melanoma (e.g., MALME-3M) and breast cancer cells (e.g., T47D) over other cancer cell lines. These results provide a method to selectively target cancers via their intrinsic need for polyamine metabolites.
