Synthetic Route of C6H7N3OIn 2015, Gladysz, Rafaela;Adriaenssens, Yves;De Winter, Hans;Joossens, Jurgen;Lambeir, Anne-Marie;Augustyns, Koen;Van der Veken, Pieter published 《Discovery and SAR of Novel and Selective Inhibitors of Urokinase Plasminogen Activator (uPA) with an Imidazo[1,2-a]pyridine Scaffold》. 《Journal of Medicinal Chemistry》published the findings. The article contains the following contents:
Urokinase plasminogen activator (uPA) is a biomarker and therapeutic target for several cancer types. Its inhibition is regarded as a promising, noncytotoxic approach in cancer therapy by blocking growth and/or metastasis of solid tumors. Earlier, the authors reported the modified substrate activity screening (MSAS) approach and applied it for the identification of fragments with affinity for uPA’s S1 pocket. Here, these fragments are transformed into a novel class of uPA inhibitors with an imidazo[1,2-a]pyridine scaffold. The SAR for uPA inhibition around this scaffold is explored, and the best compounds in the series have nanomolar uPA affinity and selectivity with respect to the related trypsin-like serine proteases (thrombin, tPA, FXa, plasmin, plasma kallikrein, trypsin, FVIIa). Finally, the approach followed for translating fragments into small mols. with a decorated scaffold architecture is conceptually straightforward and can be expected to be broadly applicable in fragment-based drug design. To complete the study, the researchers used 6-Aminonicotinamide (cas: 329-89-5) .
6-Aminonicotinamide (cas:329-89-5)Synthetic Route of C6H7N3O induces apoptosis in tumor cells. It is clinically used in disseminated neoplastic disease. It also acts as 6-phosphogluconate dehydrogenase inhibitor. It aids in the treatment of psoriasis. It is used as cancer chemotherapeutic drug in animals.
Reference:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics