On September 15, 2020, Kundu, Biswajit; Sarkar, Dipayan; Chowdhuri, Srijita Paul; Pal, Sourav; Das, Subhendu K.; Das, Benu Brata; Talukdar, Arindam published an article.Product Details of 5036-48-6 The title of the article was Development of a metabolically stable topoisomerase I poison as anticancer agent. And the article contained the following:
We have recently reported a new chemotype of a potent topoisomerase I poison with compound 1 as a potential anticancer chemotherapeutic agent. During further optimization, it has been observed that compound 1 suffers from high intrinsic clearance in human liver microsomes. To overcome the metabolic instability of compound 1, we report design and synthesis of metabolically stable Top1 poison 3. Newly identified Top1 poison 3 exhibits t1/2 of 69.1 min in human liver microsomes in comparison to compound 1 with t1/2 of 9.9 min. Mol. dynamic study of the newly optimized Top1 poison 3 was performed to get the insight into the stability of the binding pose in the active site. Compound 3 was able to trap DNA-Top1 cleavage complex and found to be less cytotoxic in non-cancerous cell line as compared to compound 1. The experimental process involved the reaction of N-(3-Aminopropyl)-imidazole(cas: 5036-48-6).Product Details of 5036-48-6
The Article related to preparation stable topoisomerase i inhibitor cancer, camptothecin, in vitro pharmacokinetics, metabolic stability, molecular dynamics, poison, topoisomerase 1, Pharmacology: Structure-Activity and other aspects.Product Details of 5036-48-6
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem