A5031024855- Cancer therapeutics and mechanisms
- Synthesis and biological activity
- Natural product bioactivities and synthesis
- NF-κB Signaling Pathways
- Genomics, phytochemicals, and oxidative stress
- Sesquiterpenes and Asteraceae Studies
- Click Chemistry and Applications
- Cancer Immunotherapy and Biomarkers
- Pharmacological Effects of Natural Compounds
- Cancer Treatment and Pharmacology
- Acute Lymphoblastic Leukemia research
- Quinazolinone synthesis and applications
- Lung Cancer Treatments and Mutations
- Genetic factors in colorectal cancer
- Melanoma and MAPK Pathways
- 14-3-3 protein interactions
- Synthesis and bioactivity of alkaloids
- Bioactive Compounds and Antitumor Agents
- Microtubule and mitosis dynamics
Aristotle University of Thessaloniki
2019-2023
Microtubule affinity regulating kinase 4 (MARK4) becomes a unique anti-cancer drug target as its overexpression is responsible for different types of cancers. In quest novel, effective MARK4 inhibitors, some acridone derivatives were synthesized, characterized and evaluated inhibitory activity against human MARK4. Among all the synthesized compounds, three (7b, 7d 7f) found to have better binding enzyme inhibition in µM range shown by fluorescence binding, ITC assays. Here we used functional...
Acridones present numerous pharmacological activities, including inhibition of microtubule affinity-regulating kinase 4 (MARK4) activity. To investigate structure–activity relationships and develop potent MARK4 inhibitors, derivatives 2-methylacridone were synthesized tested for their activity against kinase. Selective substitutions at the nitrogen atom accomplished by treating with alkyl halides in presence K2CO3. In addition, amidation acridone acetic acid 11 piperazine or tryptophan...
Bisindole alkaloids are well-known bioactive natural products presenting numerous pharmacological properties. Following the indolocarbazole biosynthetic pathway a series of bisindole derivatives were synthesized and their activity against MARK4 kinase was investigated. The binding bisindoles on measured with both fluorescence quenching ITC. Further, enzyme inhibition assays revealed that tested compounds inhibitors IC50 values in low micromolar range. inhibitory 20 33 four additional...
The fusion of 1,2,4-triazole and 1,3,4-thiadiazole rings results in a class heterocycles compounds with an extensive range pharmacological properties. A series 1,2,4-triazolo[3,4-b]-1,2,4-thiadiazoles was synthesized tested for its enzyme inhibition potential anticancer activity. show that display potent properties vitro against panel cancer cells vivo efficacy HT-29 human colon tumor xenograft CB17 severe combined immunodeficient (SCID) mice. Preliminary mechanistic studies revealed KA25...
Aim: Steroidal prodrugs of nitrogen mustards such as estramustine and prednimustine have proven effective anticancer agents in clinical use since the 1970s. In this work, we aimed to develop steroidal novel mustard POPAM-NH2. POPAM-NH2 is a melphalan analogue that was coupled with three different lactams. Methodology: The new conjugates were preclinically tested for activity against nine human one rodent cancer experimental models, vitro vivo. Results & conclusion: All alkylators showed high...
Background: Topoisomerase IIα (topIIα) maintains the topology of DNA in order to ensure proper functioning numerous processes. Inhibition topIIα leads killing cancer cells thus constituting such inhibitors as useful tools therapeutics. Triazolo[3,4- b ]thiadiazole derivatives are known for their wide range pharmacological activities while previous studies have documented vitro anticancer activity. The purpose current study was investigate if these chemical compounds can act cell-free and...
Microsatellite instability (MSI), tumor mutation burden (TMB), and programmed cell death ligand-1 (PD-L1) are particularly known as immunotherapy predictive biomarkers. MSI TMB closely related to DNA mismatch repair (MMR) pathway functionality, while the PD-L1 checkpoint mediates cancer evasion from immune surveillance via PD-L1/PD-1 axis. Among all novel triazolo[3,4-b]thiadiazole derivatives, compound KA39 emerged most potent anticancer agent. In present study, potential alterations in...