A5017188544- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Cancer therapeutics and mechanisms
- Metal complexes synthesis and properties
- Synthesis and biological activity
- Click Chemistry and Applications
- Synthesis and Characterization of Heterocyclic Compounds
- Cancer Treatment and Pharmacology
- Neuroendocrine Tumor Research Advances
- Ferrocene Chemistry and Applications
- Estrogen and related hormone effects
- Lung Cancer Research Studies
- Quinazolinone synthesis and applications
- DNA Repair Mechanisms
- Pharmacogenetics and Drug Metabolism
- Acute Lymphoblastic Leukemia research
- Computational Drug Discovery Methods
- Urinary and Genital Oncology Studies
- Cancer Immunotherapy and Biomarkers
- Protein Degradation and Inhibitors
- Bladder and Urothelial Cancer Treatments
- Histone Deacetylase Inhibitors Research
- Lung Cancer Treatments and Mutations
- PARP inhibition in cancer therapy
- Peptidase Inhibition and Analysis
National and Kapodistrian University of Athens
2012-2024
Theageneio General Hospital
2005-2017
The development of new antitumor agents is one the most pressing research areas in medicinal chemistry and medicine. importance triazole thiadiazole rings as scaffolds present a wide range therapeutic has been well reported driven synthesis large number novel agents. presence these heterocycles furnishes extensive synthetic possibilities due to several reaction sites. Prompted by data we designed, synthesized evaluated series 3,6-disubstituted 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole...
In recent years, there has been an increasing interest in the study of Ag(I) coordination compounds as potent antibacterial and anticancer agents. Herein, a series complexes bearing phosphines heterocyclic thioamide ligands with highly electronegative NH2- CF3-group substituents, i.e. [AgCl(atdztH)(xantphos)] (1), [Ag(μ-atdztH)(DPEphos)]2(NO3)2 (2), [Ag(atdzt)(PPh3)3] (3), [Ag(μ-atdzt)(DPEphos)]2 (4), [Ag(μ-mtft)(DPEphos)]2 (5), where atdztH = 5-amino-1,3,4-thiadiazole-2-thiol, mtftH...
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...
Alkylating agents and antimetabolites are cytotoxic drugs commonly used in cancer treatment. These medications often associated with serious side effects on normal tissues organs.To improve the pharmacological profile of alkylating agent POPAM antimetabolite 5-fluorouracil, novel integrin-targeted delivery systems based c(RGDyK) were successfully synthesized. The new conjugates tested vitro against different cells such as PC3, SKOV3, A549, MCF7 MBA-MB-321.The demonstrated better inhibitory...
Ag(I) coordination compounds have recently attracted much attention as antiproliferative and antibacterial agents against a wide range of cancer cell lines pathogens. The bioactivity potential these complexes depends on their structural characteristics the nature ligands. Herein, we present series four bearing ligands CH3-substituted thiadiazole-based thioamide 5-methyl-1,3,4-thiadiazole-2-thiol (mtdztH) phosphines, i.e., [AgCl(mtdztH)(PPh3)2] (1), [Ag(mtdzt)(PPh3)3] (2),...
It is widely known that ionizing irradiation strongly linked to the production of reactive oxygen (ROS) and nitrative species (RNS) through which DNA damage products like 8-hydroxy-2-deoxyguanosine (8-OHdG) 8-nitroguanine (8-NG) are generated, respectively. In present study, we aimed investigate formation 8-OHdG 8-NG upon further explore whether alterations in their concentration levels related administered radiation doses exposure time. Our research work was conducted blood serum samples...
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...
Cucurbitacins (CUCUs) are triterpenoids known to display potent cytotoxic effects; however, their clinical application is limited due poor pharmacokinetics and systemic toxicity. This work focuses on the development of c(RGDyK)–CUCU conjugates for selective delivery CUCUs integrin-overexpressing cancer cells. The activity against various cells was studied. They exhibited a mild cytostatic effect six cell lines MCF-7 A549 Their chemical metabolic stability extensively studied using LC–MS...
Conjugated lactam‐steroid alkylators (LSA) have been shown to exhibit superior activity at controlling cancer models and overlap drug resistance conventional chemjournalapy. Hybrid LSA combine two active compounds in a single molecule incorporate modified steroids bearing lactam moiety one or more steroid rings functioning as vectors for cytotoxic agents. We first describe novel class of that generate excellent anticancer against UWB1.289 + BRCA1 human ovarian cell lines. Both cells carry...
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...
Summary NSC290205 (A) is an hybrid synthetic antineoplastic ester that a combination of d-lactam derivative androsterone and alkylating N,N-bis(2-chloroethyl)aniline. We tested for synergistic antileukaemic activity with adriamycin (ADR), (i) in vitro against the human lymphoid leukaemia cell lines: CCRF-CEM, MOLT-4, RPMI-8226, (ii) vivo P388 lymphocytic L1210 murine leukaemias (at incipient advanced phase). Our results indicated significant cytostatic cytotoxic synergy ADR vitro. further...