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[ CAS No. 492-73-9 ] {[proInfo.proName]}

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Chemical Structure| 492-73-9
Chemical Structure| 492-73-9
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Premnauth, Gurdat ;

Abstract: Cancer remains one of the leading causes of mortality in the world. Even with the improvement of treatments in multiple type of cancer, current chemotherapies are highly toxic and associated with severe acute side effects due to the low selectivity of the existing drugs. Additionally, multiple cancers develop chemotherapeutic resistance and new targets need to be investigated. Amongst them, Ras is one of the most common aberration found in cancer with approximately 30% of cancer containing the mutated oncogenes. Rastargeted therapy with small molecule inhibitor could be the key to better and safer treatments. Moreover, the use of targeted therapy with drug conjugate and delivery vehicles such as aptamers, antibodies or targeting peptides could help bring selectivity to treatments and reduce off-target toxicity. This dissertation focuses on the development of both targeted therapy strategies for cancer treatment. In the first half, we report the identification of IODVA1 as the active compound of NSC124205 for the treatment of Ras-driven cancer models in cellulo and in vivo. Identification of the IDOVA1 side products led me to synthesize GUPR-195 followed by the synthesis of several related molecules. In the other half, we focus on decreasing toxic off-target inhibitors effect using targeting therapy. Here, we developed two new reactive oxygen species (ROS)-sensitive linkers for selective drug release to leukemic cells. Indeed, cancer cells are known to have higher levels of ROS than their healthy counterparts. By using a ROS-sensitive linker for the conjugation of a cytotoxic payload to a delivery vehicle, it is possible to double the selectivity of drug release. We report in the last chapter of the dissertation the development of a self-cyclizing ROS-sensitive linker and an oxalamide ROS-sensitive linker.

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Product Details of [ 492-73-9 ]

CAS No. :492-73-9 MDL No. :MFCD00006301
Formula : C12H8N2O2 Boiling Point : -
Linear Structure Formula :(CO)2(C5H4N)2 InChI Key :PIINXYKJQGMIOZ-UHFFFAOYSA-N
M.W : 212.20 Pubchem ID :68115
Synonyms :

Safety of [ 492-73-9 ]

Signal Word:Warning Class:N/A
Precautionary Statements:P261-P305+P351+P338 UN#:N/A
Hazard Statements:H315-H319-H335 Packing Group:N/A
GHS Pictogram:

Application In Synthesis of [ 492-73-9 ]

* All experimental methods are cited from the reference, please refer to the original source for details. We do not guarantee the accuracy of the content in the reference.

  • Downstream synthetic route of [ 492-73-9 ]

[ 492-73-9 ] Synthesis Path-Downstream   1~1

  • 1
  • [ 492-73-9 ]
  • [ 62-53-3 ]
  • [ 110677-45-7 ]
  • 9-(4-(1-phenyl-4,5-di(pyridin-2-yl)-1H-imidazol-2-yl)phenyl)-9H-carbazole [ No CAS ]
YieldReaction ConditionsOperation in experiment
46% With ammonium acetate; acetic acid; at 120℃; for 12h; General procedure: 4-(10H-phenoxazin-10-yl)benzaldehyde (0.4 g, 1.39 mmol), 1,2-di(pyridin-2-yl)ethane-1,2-dione (0.295 g, 1.39 mmol), aniline (0.65 g, 6.96 mmol), ammonium acetate (1.33 g,17.26 mmol), and acetic acid (9 mL) were mixed in a flask and heated under 120 reflux for 12 h. After the completion of the reaction, the reaction mixture was extracted with CHCl3 and washed with water. The organic layer was dried over anhydrous MgSO4 and filtered through celite. Then, the solution was evaporated, and the residue was purifiedby column chromatography on silica gel using dichloromethane/hexane as the eluent.
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