[HTML][HTML] Transdermal drug delivery

MR Prausnitz, R Langer - Nature biotechnology, 2008 - nature.com
Transdermal drug delivery has made an important contribution to medical practice, but has
yet to fully achieve its potential as an alternative to oral delivery and hypodermic injections …

Measuring and interpreting the selectivity of protein kinase inhibitors

LA Smyth, I Collins - Journal of chemical biology, 2009 - Springer
Protein kinase inhibitors are a well-established class of clinically useful drugs, particularly
for the treatment of cancer. Achieving inhibitor selectivity for particular protein kinases often …

CR8, a potent and selective, roscovitine-derived inhibitor of cyclin-dependent kinases

K Bettayeb, N Oumata, A Echalier, Y Ferandin… - Oncogene, 2008 - nature.com
Among the ten pharmacological inhibitors of cyclin-dependent kinases (CDKs) currently in
clinical trials, the purine roscovitine (CYC202, Seliciclib) is undergoing phase 2 trials against …

Isatin-hydrazide conjugates as potent α-amylase and α-glucosidase inhibitors: Synthesis, structure and in vitro evaluations

I Abbasi, H Nadeem, A Saeed, HAA Kharl, MN Tahir… - Bioorganic …, 2021 - Elsevier
Managing diabetes that is a global life-threatening problem, remains a challenge for the
scientific community. The inhibition of α-amylase and α-glucosidase enzymes which are …

Roscovitine-derived, dual-specificity inhibitors of cyclin-dependent kinases and casein kinases 1

N Oumata, K Bettayeb, Y Ferandin… - Journal of medicinal …, 2008 - ACS Publications
Cyclin-dependent kinases (CDKs) and casein kinases 1 (CK1) are involved in the two key
molecular features of Alzheimer's disease, production of amyloid-β peptides (extracellular …

Indole-fused azepines and analogues as anticancer lead molecules: privileged findings and future directions

AK Singh, V Raj, S Saha - European journal of medicinal chemistry, 2017 - Elsevier
The search for new lead compounds of simple structure, displaying highest quality anti-
tumor potency with new mechanisms of action and least adverse effects is the major …

Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolin complex

A Echalier, K Bettayeb, Y Ferandin… - Journal of medicinal …, 2008 - ACS Publications
We report the synthesis and biological characterization of 3-(pyrimidin-4-yl)-7-azaindoles
(meriolins), a chemical hybrid between the natural products meridianins and variolins …

Meriolins, a new class of cell death–inducing kinase inhibitors with enhanced selectivity for cyclin-dependent kinases

K Bettayeb, OM Tirado, S Marionneau-Lambot… - Cancer Research, 2007 - AACR
Protein kinases represent promising anticancer drug targets. We describe here the
meriolins, a new family of inhibitors of cyclin-dependent kinases (CDK). Meriolins represent …

Design, synthesis and biological evaluation of certain CDK2 inhibitors based on pyrazole and pyrazolo [1, 5-a] pyrimidine scaffold with apoptotic activity

GME Ali, DA Ibrahim, AM Elmetwali, NSM Ismail - Bioorganic Chemistry, 2019 - Elsevier
Different series of novel pyrazole and pyrazolo [1, 5-a] pyrimidine derivatives (2a-g),(3a-
c),(7a-d) and (10a-e) were designed, synthesized and evaluated for their ability to inhibit …

CDK inhibitors roscovitine and CR8 trigger Mcl-1 down-regulation and apoptotic cell death in neuroblastoma cells

K Bettayeb, D Baunbæk, C Delehouze… - Genes & …, 2010 - journals.sagepub.com
Neuroblastoma (NB), the most frequent extracranial solid tumor of children accounting for
nearly 15% of all childhood cancer mortality, displays overexpression of antiapoptotic Bcl-2 …