Triazolopyrimidine and triazolopyridine scaffolds as TDP2 inhibitors was written by Ribeiro, Carlos J. A.;Kankanala, Jayakanth;Xie, Jiashu;Williams, Jessica;Aihara, Hideki;Wang, Zhengqiang. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2019.SDS of cas: 1711-11-1 This article mentions the following:
Tyrosyl-DNA phosphodiesterase 2 (TDP2) repairs topoisomerase II (TOP2) mediated DNA damages and causes cellular resistance to clin. used TOP2 poisons. Inhibiting TDP2 can potentially sensitize cancer cells toward TOP2 poisons. Com. compound P10A10, to which the structure was assigned as 7-Ph triazolopyrimidine analog 6a, was previously identified as a TDP2 inhibitor hit in our virtual and fluorescence-based biochem. screening campaign. We report herein that the hit validation through resynthesis and structure elucidation revealed the correct structure of P10A10 (Chembridge ID 7236827) to be the 5-Ph triazolopyrimidine regioisomer 7a. Subsequent structure-activity relationship (SAR) via the synthesis of a total of 47 analogs of both the 5-Ph triazolopyrimidine scaffold (7) and its bioisosteric triazolopyridine scaffold (17) identified four derivatives (7a, 17a, 17e, and 17z) with significant TDP2 inhibition (IC50 < 50 μM), with 17z(I) showing excellent cell permeability and no cytotoxicity. In the experiment, the researchers used many compounds, for example, 3-Cyanobenzoyl chloride (cas: 1711-11-1SDS of cas: 1711-11-1).
3-Cyanobenzoyl chloride (cas: 1711-11-1) belongs to organic chlorides. An organic chloride is an organic compound containing at least one covalently bonded atom of chlorine. Their wide structural variety and divergent chemical properties lead to a broad range of names and applications. Alkyl chlorides are versatile building blocks in organic chemistry. While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available.SDS of cas: 1711-11-1
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics