A5043038313- Bioactive Compounds and Antitumor Agents
- Cancer-related Molecular Pathways
- Protein Tyrosine Phosphatases
- Protein Kinase Regulation and GTPase Signaling
- Synthesis and Reactivity of Heterocycles
- Monoclonal and Polyclonal Antibodies Research
- Cancer therapeutics and mechanisms
- Microbial Metabolites in Food Biotechnology
- HIV/AIDS drug development and treatment
- Synthesis and biological activity
- HIV Research and Treatment
- Cell death mechanisms and regulation
- Microbial Natural Products and Biosynthesis
- Synthesis and bioactivity of alkaloids
- Natural Antidiabetic Agents Studies
- 14-3-3 protein interactions
Latakia University
2016-2024
Université Claude Bernard Lyon 1
2015-2021
Centre National de la Recherche Scientifique
2015-2021
Inserm
2015-2021
Manara University
2021
Laboratoire de Chémo-biologie synthétique et thérapeutique
2021
Centre Orthopédique Santy
2021
Due to their system of annulated 6-5-5-6-membered rings, indenoindoles have sparked great interest for the design ATP-competitive inhibitors human CK2. In present study, we prepared twenty-one indeno[1,2-b]indole derivatives, all which were tested in vitro on The indenoindolones 5a and 5b inhibited CK2 with an IC50 0.17 0.61 µM, respectively. indeno[1,2-b]indoloquinone 7a also showed inhibitory activity at a submicromolar range (IC50 = 0.43 µM). Additionally, large number indenoindole...
Quinones and quinones-like compounds are potential candidates for the inhibition of CDC25 phosphatases. The combination MALDI-MS analyses biological studies was used to develop a rapid screening targeted library indeno[1,2-b]indoloquinone derivatives. protocol using MALDI-TOFMS MALDI-FTICRMS highlighted four new promising candidates. Biological investigations showed that only 5c–f inhibited CDC25A -C phosphatases, with IC50 values around micromolar range. direct use method based on...
Highly pleiotropic and constitutively active protein kinase CK2 is a key target in cancer therapy, but only one small‐molecule inhibitor has reached clinical trials—CX‐4945. In this study, we present the indeno[1,2‐ b ]indole derivative 5‐isopropyl‐4‐methoxy‐7‐methyl‐5,6,7,8‐tetrahydroindeno[1,2‐ ]indole‐9,10‐dione ( 5a‐2 ) that decreased intracellular activity A431, A549, LNCaP tumor cell lines analogous to CX‐4945 (> 75% inhibition at 20 µ m similarly blocked CK2‐specific Akt...
Abstract Acquired Immunodeficiency Syndrome (AIDS) is a chronic and potentially fatal transmissible disease caused by the Human Virus (HIV). Since its discovery in 1981, an estimated 85 million cases 40 AIDS related deaths have occurred worldwide. Among two types of HIV, HIV-1 accounts for over 90% reported cases. Throughout years, multiple drugs been approved treatment AIDS. However, these face many drawbacks such as toxic side effects, non-optimal pharmacokinetic profile drug resistance...
The highly pleiotropic and constitutively active serine/threonine protein kinase CK2 is considered a key target in cancer. indeno[1,2-b]indole scaffold was previously shown to provide derivatives exhibiting strong inhibition satisfactory drug-like characteristics. In this work, we evaluated one 4,5,7-trisubstituted derivative for its intracellular of activity the accompanying effects on proliferation, migration apoptosis cancer cells. compound...
Diabetes mellitus is a serious disease that threatens human health. The most prevalent type of diabetes 2 (T2DM) which characterized by the lack insulin secretion and resistance to in target tissues. Protein Tyrosine Phosphatase 1B (PTP1B) plays an important role dephosphorylation phospho-tyrosine residues from receptor its substrate. Studies have shown overexpression PTP1B protein increased activation been associated with thus it promising therapeutic for diabetes. discovery selective...
Casein kinase 2 (CK2) is a highly pleiotropic serine/threonine protein whose list of substrates includes >300 proteins implicated in wide variety cell functions. The catalytic subunits CK2 (alpha and/or alpha') are constitutively active either alone or combination with the regulatory beta-subunits to give heterotetrameric protein. High constitutive activity related contribute cancer. Based on recent years effort, German French collaborative network has developed indeno[1,2-b]indole scaffold...