2009
DOI: 10.1016/j.bmcl.2009.09.069
|View full text |Cite
|
Sign up to set email alerts
|

Design, synthesis and bioevaluation of novel maleamic amino acid ester conjugates of 3,5-bisarylmethylene-4-piperidones as cytostatic agents

Help me understand this report

Search citation statements

Order By: Relevance

Paper Sections

Select...
3
1

Citation Types

0
11
0

Year Published

2010
2010
2015
2015

Publication Types

Select...
5

Relationship

2
3

Authors

Journals

citations
Cited by 9 publications
(11 citation statements)
references
References 27 publications
0
11
0
Order By: Relevance
“…[22] Briefly, the energy of the molecular structure of the compound was minimized using Merck Molecular Force Field (MMFF94). Atomic charges were obtained using extended Hückel method.…”
Section: Statistical Analysesmentioning
confidence: 99%
See 3 more Smart Citations
“…[22] Briefly, the energy of the molecular structure of the compound was minimized using Merck Molecular Force Field (MMFF94). Atomic charges were obtained using extended Hückel method.…”
Section: Statistical Analysesmentioning
confidence: 99%
“…Notably, the analogs from series 5-10 contain additional enone moiety in their side chains bearing for interaction with auxiliary binding domain [20] and/or protein thiolation [25,28]. We have identified human topoisomerase IIα as a potential molecular target for 3,5-bisarylmethylene-4-piperidone derivatives [22]. This thiol-rich enzyme is essential for sustained cell proliferation [29][30][31].…”
Section: Introductionmentioning
confidence: 97%
See 2 more Smart Citations
“…A number of studies report that protein thiolation plays an important role in biochemical processes. Some representative examples of this phenomenon include inhibition of human cytomegalovirus protease, 16 inhibition of Ref-1, a therapeutic target for asthma, 17 inactivation of cysteine proteases, 18 blockade of platelet-derived growth factor BB-stimulated Akt phosphorylation, 19 catalytic inhibition of human topoisomerase-2 alpha, an established target for the development of anticancer agents, 20,21 etc. This encouraged us the study the reactivity of representative compounds in each of the series 1 – 5 and 9 towards a model thiol, benzyl mercaptan, under simulated physiological conditions These experiments were undertaken in order to evaluate whether the compounds in these series are in fact thiol alkylators and, if so, to determine the locus of thiolation.…”
mentioning
confidence: 99%