- A benzofuran-β-Alaninamide based "turn-on" fluorescent chemosensor for selective recognition of Fe3+ ions
-
A benzofuran-β-Alaninamide based chemosensor, 3-(3-((4-methylbenzyl)amino)propanamido)benzofuran-2-carboxamide (BAA), was designed and synthesized for selective detection of Fe3+ ions. The binding ability of BAA towards Fe3+ in DMSO/
- Madhu,Sivakumar,Sribalan, Rajendran
-
p. 14426 - 14434
(2019/09/30)
-
- The design, synthesis, and biological evaluation of PIM kinase inhibitors
-
A series of substituted benzofuropyrimidinones with pan-PIM activities and excellent selectivity against a panel of diverse kinases is described. Initial exploration identified aryl benzofuropyrimidinones that were potent, but had cell permeability limitation. Using X-ray crystal structures of the bound PIM-1 complexes with 3, 5m, and 6d, we were able to guide the SAR and identify the alkyl benzofuropyrimidinone (6l) with good PIM potencies, permeability, and oral exposure.
- Tsuhako, Amy Lew,Brown, David S.,Koltun, Elena S.,Aay, Naing,Arcalas, Arlyn,Chan, Vicky,Du, Hongwang,Engst, Stefan,Franzini, Maurizio,Galan, Adam,Huang, Ping,Johnston, Stuart,Kane, Brian,Kim, Moon H.,Douglas Laird,Lin, Rui,Mock, Lillian,Ngan, Iris,Pack, Michael,Stott, Gordon,Stout, Thomas J.,Yu, Peiwen,Zaharia, Cristiana,Zhang, Wentao,Zhou, Peiwen,Nuss, John M.,Kearney, Patrick C.,Xu, Wei
-
p. 3732 - 3738
(2012/07/17)
-
- Discovery of XL413, a potent and selective CDC7 inhibitor
-
CDC7 is a serine/threonine kinase that has been shown to be required for the initiation and maintenance of DNA replication. Up-regulation of CDC7 is detected in multiple tumor cell lines, with inhibition of CDC7 resulting in cell cycle arrest. In this paper, we disclose the discovery of a potent and selective CDC7 inhibitor, XL413 (14), which was advanced into Phase 1 clinical trials. Starting from advanced lead 3, described in a preceding communication, we optimized the CDC7 potency and selectivity to demonstrate in vitro CDC7 dependent cell cycle arrest and in vivo tumor growth inhibition in a Colo-205 xenograft model.
- Koltun, Elena S.,Tsuhako, Amy Lew,Brown, David S.,Aay, Naing,Arcalas, Arlyn,Chan, Vicky,Du, Hongwang,Engst, Stefan,Ferguson, Kim,Franzini, Maurizio,Galan, Adam,Holst, Charles R.,Huang, Ping,Kane, Brian,Kim, Moon H.,Li, Jia,Markby, David,Mohan, Manisha,Noson, Kevin,Plonowski, Arthur,Richards, Steven J.,Robertson, Scott,Shaw, Kenneth,Stott, Gordon,Stout, Thomas J.,Young, Jenny,Yu, Peiwen,Zaharia, Cristiana A.,Zhang, Wentao,Zhou, Peiwen,Nuss, John M.,Xu, Wei,Kearney, Patrick C.
-
scheme or table
p. 3727 - 3731
(2012/07/16)
-
- HCV PROTEASE INHIBITORS
-
This invention relates to compounds of Formula (I), (II), or (III) shown in the specification. These compounds can be used to treat hepatitis C virus infection.
- -
-
-
- Syntheses of 3-acetoacetylaminobenzo[b]furan derivatives having cysteinyl leukotriene 2 receptor antagonistic activity
-
Novel 3-acetoacetylaminobenzo[b]furan derivatives having a modified triene system at the 3-position were synthesized starting with 3-aminobenzo[b]furans. The enol isomers, 3-[(3-hydroxybul-2-enonyl)amino]benzo[b]furans (1), of the 3-acetoacetylaminobenzo[b]furans were obtained as stable isomers owing to formation of a hydrogen bonding between the enol hydroxyl group and the amidocarbonyl group. The planarity of the C-2 substituent through the C-3 side chain suggested the existence of a modified conjugational triene system in the enol compound. Cysteinyl leukotriene 1 and 2 receptor antagonistic activities for these compounds were evaluated. 2-(4-Cyanobenzoyl or ethoxycarbonyl)-3-[(2-cyano-3-hydroxybut-2-enonyl)amino]benzo[e]furans (15g, 15o, 15u) were moderately active.
- Ando, Kumiko,Tsuji, Eriko,Ando, Yuko,Kuwata, Noriko,Kunitomo, Jun-Ichi,Yamashita, Masayuki,Ohta, Shunsaku,Kohno, Shigekatsu,Ohishi, Yoshitaka
-
p. 625 - 635
(2007/10/03)
-
- 3-thio or amino substituted-benzo[b]thiophene-2-carboxamides and 3-oxygen, thio, or amino substituted-benzofuran-2-carboxamides as inhibitors of cell adhesion
-
3-Thio or amino substituted benzo[b]thiophene-2-carboxamides and 3-oxygen, thio, or amino substituted benzofuran-2-carboxamides are described as agents which inhibit leukocyte adherence to vascular endothelium and, as such, are effective therapeutic agent
- -
-
-
