The author of 《Design, synthesis and biological evaluation of pentacyclic triterpene derivatives: optimization of anti-ABL kinase activity》 were Ciftci, Halil I.; Radwan, Mohamed O.; Ozturk, Safiye E.; Ulusoy, N. Gokce; Sozer, Ece; Ellakwa, Doha E.; Ocak, Zeynep; Can, Mustafa; Ali, Taha F. S.; Abd-Alla, Howaida I.; Yayli, Nurettin; Tateishi, Hiroshi; Otsuka, Masami; Fujita, Mikako. And the article was published in Molecules in 2019. Application In Synthesis of 4-Cyanobenzyl bromide The author mentioned the following in the article:
Imatinib, an Abelson (ABL) tyrosine kinase inhibitor, is a lead mol.-targeted drug against chronic myelogenous leukemia (CML). To overcome its resistance and adverse effects, new inhibitors of ABL kinase are needed. Our previous study showed that the benzyl ester of gypsogenin (1c), a pentacyclic triterpene, has anti-ABL kinase and a subsequent anti-CML activity. To optimize its activities, benzyl esters of carefully selected triterpenes (PT1-PT6), from different classes comprising oleanane, ursane and lupane, and new substituted benzyl esters of gypsogenin (GP1-GP5) were synthesized. All of the synthesized compounds were purified and charachterized by different spectroscopic methods. Cytotoxicity of the parent triterpenes and the synthesized compounds against CML cell line K562 was examined; revealing three promising compounds PT5, GP2 and GP5 (IC50 5.46, 4.78 and 3.19 microM, resp.). These compounds were shown to inhibit extracellular signal-regulated kinase (ERK) downstream signaling, and induce apoptosis in K562 cells. Among them, PT5 was identified to have in vitro activity (IC50 = 1.44 microM) against ABL1 kinase, about sixfold of 1c, which was justified by mol. docking. The in vitro activities of GP2 and GP5 are less than PT5, hence they were supposed to possess other more mechanisms of cytotoxicity. In general, our design and derivatizations resulted in enhancing the activity against ABL1 kinase and CML cells. The experimental part of the paper was very detailed, including the reaction process of 4-Cyanobenzyl bromide(cas: 17201-43-3Application In Synthesis of 4-Cyanobenzyl bromide)
4-Cyanobenzyl bromide(cas: 17201-43-3) is an important intermediate for pharmaceutical production. It can be used for the synthesis of a series of piperidine-linked aromatic diimidazolines, which have been synthesized as conformationally restricted congeners of the anti-Pneumocystis carinii (PCP) drug, Pentamidine.Application In Synthesis of 4-Cyanobenzyl bromide
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts