Show simple item record

dc.contributor.authorQhobosheane, Malikotsi A.
dc.contributor.authorLegoabe, Lesetja J.
dc.contributor.authorBeteck, Richard M.
dc.contributor.authorJosselin, Béatrice
dc.contributor.authorBach, Stéphane
dc.date.accessioned2020-08-28T09:20:34Z
dc.date.available2020-08-28T09:20:34Z
dc.date.issued2020
dc.identifier.citationQhobosheane, M.A. et al. 2020. Synthesis and evaluation of C3 substituted chalcone-based derivatives of 7-azaindole as protein kinase inhibitors. Chemical biology and drug design, (In press). [https://doi.org/10.1111/cbdd.13748]en_US
dc.identifier.issn1747-0277
dc.identifier.issn1747-0285 (Online)
dc.identifier.urihttp://hdl.handle.net/10394/35652
dc.identifier.urihttps://onlinelibrary.wiley.com/doi/10.1111/cbdd.13748
dc.identifier.urihttps://doi.org/10.1111/cbdd.13748
dc.description.abstractChalcones are a group of naturally occurring or synthetic compounds which possess a wide range of biological activities. In this paper, a series of twenty‐three 7‐azaindole‐chalcone hybrids (5a–w) were synthesized and evaluated as potential protein kinase inhibitors. Analyses of structure–activity relationships revealed that some of these compounds exhibit significant activity against Haspin kinase, with compounds 5f and 5q exhibiting IC50 values of 0.47 and 0.41 µM, respectively. Furthermore, 5f also inhibits cyclin‐dependent kinase 9 (CDK9/CyclinT) in a micromolar potency (IC50 = 2.26 µM). This novel dual‐target inhibitor is a promising lead for the development of chemopreventive/chemotherapeutic agentsen_US
dc.language.isoenen_US
dc.publisherWileyen_US
dc.subject7‐Azaindoleen_US
dc.subjectCDK9/CyclinTen_US
dc.subjectChalconeen_US
dc.subjectDual inhibitoren_US
dc.subjectHaspinen_US
dc.subjectProtein kinaseen_US
dc.subjectStructure-activity relationshipsen_US
dc.titleSynthesis and evaluation of C3 substituted chalcone-based derivatives of 7-azaindole as protein kinase inhibitorsen_US
dc.typeArticleen_US
dc.contributor.researchID12902608 - Legoabe, Lesetja Jan
dc.contributor.researchID25159194 - Beteck, Richard Mbi
dc.contributor.researchID27836576 - Qhobosheane, Malikotsi A.


Files in this item

FilesSizeFormatView

There are no files associated with this item.

This item appears in the following Collection(s)

Show simple item record