Tetrahedron p. 9847 - 9864 (1994)
Update date:2022-08-04
Topics:
Neder, Karen M.
French, Stephanie A.
Miller, Stephen P. F.
Two fluorinatednonhydrolyzable analogs of myristoyl-coenzyme A were synthesized and tested for inhibitory activity against N-myristoyltransferase (NMT).S-(2,2-Difluoro-3-oxohexadecyl)-coenzyme A (3) and S-(3,3-difluoro-2-oxopentadecyl)-coenzyme A (2) were prepared by alkylation of coenzyme A and were purified by reverse phase chromatography.Inhibition of NMT was observed with 3 and 2, with IC50's of 110 nM and 80 nM, respectively, in an in vitro assay developed in our laboratory.The known unfluorinated analog S-(2-oxopentadecyl)-coenzyme A (1) was found to have an IC50 of 7 nM.At 100 μM in D2O, 3 was 59percent hydrated and 2 was 88percent hydrated.
View MoreShanghai Sinofluoro Scientific Co., Ltd
Contact:+86-21-64279360
Address:Room 1006,Building 3,#58 East Xinjian Road, Shanghai ,201100,China,
website:http://www.maisonchem.com.cn
Contact:0086-311-83833777
Address:Leitou industrial district, xinji, shijiazhuang city, hebei province,
Liaoyang Xinyou Chemical Products Co.,Ltd.
Contact:+86-419-5165433 13604191870
Address:Huishang Road6-1, Hongwei District, Liaoyang, Liaoning, China
JiYi Chemical (Beijing) Co., Ltd.
Contact:+86-10-89385733
Address:Shilou Town of Fangshan District， Beijing
Contact:86-27-84888681
Address:Wuhan economic & technology development zone
Doi:10.1021/ja909962f
(2010)Doi:10.1007/s10593-009-0343-2
(2009)Doi:10.1002/1522-2675(200201)85:1<255::AID-HLCA255>3.0.CO;2-5
(2002)Doi:10.1016/j.apcata.2014.01.002
(2014)Doi:10.1016/S0040-4039(00)98217-0
(1985)Doi:10.1002/anie.201605584
(2016)
