2022
DOI: 10.1002/cmdc.202200400
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Prodrugs of the Archetypal Dynamin Inhibitor Bis‐T‐22

Abstract: The Bis‐T series of compounds comprise some of the most potent inhibitors of dynamin GTPase activity yet reported, e. g., (2E,2′E)‐N,N′‐(propane‐1,3‐diyl)bis(2‐cyano‐3‐(3,4‐dihydroxyphenyl)acrylamide) (2), Bis‐T‐22. The catechol moieties are believed to limit cell permeability, rendering these compounds largely inactive in cells. To solve this problem, a prodrug strategy was envisaged and eight ester analogues were synthesised. The shortest and bulkiest esters (acetate and butyl/tert‐butyl) were found to be in… Show more

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Cited by 1 publication
(2 citation statements)
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“…Despite its strong activity against dynamin, it had a weak effect on CME inhibition. The new prodrug of Bis-T-22 inhibits CME with an IC50 of 8.0 ± 0.5µM [ 223 ].…”
Section: Endocytosis Inhibitors: Mode Of Actionmentioning
confidence: 99%
See 1 more Smart Citation
“…Despite its strong activity against dynamin, it had a weak effect on CME inhibition. The new prodrug of Bis-T-22 inhibits CME with an IC50 of 8.0 ± 0.5µM [ 223 ].…”
Section: Endocytosis Inhibitors: Mode Of Actionmentioning
confidence: 99%
“…Despite its strong activity against dynamin, it had a weak effect on CME inhibition. The new prodrug of Bis-T-22 inhibits CME with an IC50 of 8.0 ± 0.5µM [223]. Room-temperature ionic liquid (RTIL) is a substance derived from the Spanish fly aphrodisiac cantharidin.…”
Section: Dimeric Tyrphostins (Bis-t)mentioning
confidence: 99%