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Chemical Structure| 5418-95-1 Chemical Structure| 5418-95-1

Structure of 2-Guanidinobenzimidazole
CAS No.: 5418-95-1

Chemical Structure| 5418-95-1

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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 [ 2-Guanidinobenzimidazole ]

CAS No. :5418-95-1
Formula : C8H9N5
M.W : 175.19
SMILES Code : NC(NC1=NC2=CC=CC=C2N1)=N
MDL No. :MFCD00005590
InChI Key :JJWCTKUQWXYIIU-UHFFFAOYSA-N
Pubchem ID :36149

Safety of [ 2-Guanidinobenzimidazole ]

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

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