scholarly journals Anticancer Activity of New 1,2,3-Triazole-Amino Acid Conjugates

Molbank ◽  
10.3390/m1204 ◽  
2021 ◽  
Vol 2021 (2) ◽  
pp. M1204
Author(s):  
Thanh Thanh Le ◽  
Phung Thi Kim Le ◽  
Hai Thi Thanh Dam ◽  
Duy Duc Vo ◽  
Thanh Tin Le
Keyword(s):  
Amino Acid ◽  
Cancer Cells ◽  
Mild Condition ◽  
Antiproliferative Activity ◽  
Good Yield ◽  
Amino Acid Conjugates ◽  
Multistep Synthesis ◽  
Spectroscopic Analyses ◽  
Diaryl Ether ◽  
Snar Reaction

A multistep synthesis was developed to prepare new 1,2,3-triazole-amino acid conjugates (6 and 7). These compounds contain the diaryl ether moiety and were synthesized via SNAr reaction under mild condition and in good yield. Their structures were confirmed by spectroscopic analyses (HR-MS, NMR, IR). These compounds showed significant antiproliferative activity (>30%) toward the breast MCF7 and liver HepG2 cancer cells lines at <10 µM concentration.

scholarly journals Lipoamino Acid-Modified GnRH Analogs with Receptor-Mediated Antiproliferative Activity in Prostate and Ovarian Cancer Cells

2021 ◽  
Author(s):  
Pegah Varamini ◽  
Kimmi Dhiman ◽  
Sepideh Khazeni ◽  
Frieda Mansfeld ◽  
Istvan Toth
Keyword(s):  
Ovarian Cancer ◽  
Amino Acid ◽  
Cancer Cells ◽  
Amino Acid Substitution ◽  
Anticancer Agents ◽  
Antiproliferative Activity ◽  
Gnrh Receptor ◽  
Ovarian Cancer Cells ◽  
Gnrh Analogs ◽  
Reproductive Cancers

Abstract Gonadotropin-releasing hormone (GnRH) analogs (e.g., triptorelin) are developed to treat hormone-dependent reproductive cancers. However, these analogs lack any significant direct antitumor activity to make them suitable for hormone-refractory reproductive cancers. In this study, we modified GnRH peptide and triptorelin to improve their stability, pharmacokinetic properties, and potency and subsequently broaden their clinical applications in cancer. We investigated biological properties of lipid-modified GnRH analogs, with/without D-amino acid substitution at position 6 to yield GnRH- and triptorelin-based derivatives, respectively, in prostate and ovarian cancer cells. We showed that the improved stability due to lipid-modification and D-amino acid substitution played a pivotal role in enhancing GnRH receptor-mediated direct antiproliferative activity (up to 4.5-fold higher than triptorelin) and gonadotropin-releasing potency. Furthermore, sex steroids played significant but contrasting roles in regulating the direct antiproliferative activity of the lipopeptides in cancer cells. The superior activity of these GnRH analogs over triptorelin renders promises for developing new GnRH receptor ligands to treat hormone-dependent and -refractory cancers, as well as emerging new targeting moieties for the delivery of anticancer agents in GnRH receptor-overexpressing cancers.

Selective antiproliferative activity of spinasterol from Physospemum verticillatum against A549 and COR-L23 cancer cells

Planta Medica ◽  
2012 ◽  
Vol 78 (11) ◽  
Author(s):  
R Tundis ◽  
B Deguin ◽  
MR Loizzo ◽  
M Bonesi ◽  
S Michel ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Antiproliferative Activity

Fluoroquinolone-3-carboxamide Amino Acid Conjugates: Synthesis, Antibacterial Properties And Molecular Modeling Studies

2020 ◽  
Vol 17 (1) ◽  
pp. 71-84
Author(s):  
Riham M. Bokhtia ◽  
Siva S. Panda ◽  
Adel S. Girgis ◽  
Hitesh H. Honkanadavar ◽  
Tarek S. Ibrahim ◽  
...  
Keyword(s):  
Experimental Data ◽  
Antibacterial Activity ◽  
Amino Acid ◽  
Bacterial Infections ◽  
Antibacterial Agents ◽  
Antibacterial Properties ◽  
Computational Studies ◽  
Protecting Group ◽  
Amino Acid Conjugates ◽  
Molecular Modeling Studies

Background: Bacterial infections are considered as one of the major global health threats, so it is very essential to design and develop new antibacterial agents to overcome the drawbacks of existing antibacterial agents. Method: The aim of this work is to synthesize a series of new fluoroquinolone-3-carboxamide amino acid conjugates by molecular hybridization. We utilized benzotriazole chemistry to synthesize the desired hybrid conjugates. Result: All the conjugates were synthesized in good yields, characterized, evaluated for their antibacterial activity. The compounds were screened for their antibacterial activity using methods adapted from the Clinical and Laboratory Standards Institute. Synthesized conjugates were tested for activity against medically relevant pathogens; Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27856) Staphylococcus aureus (ATCC 25923) and Enterococcus faecalis (ATCC 19433). Conclusion: The observed antibacterial experimental data indicates the selectivity of our synthesized conjugates against E.Coli. The protecting group on amino acids decreases the antibacterial activity. The synthesized conjugates are non-toxic to the normal cell lines. The experimental data were supported by computational studies.

scholarly journals The Antiproliferative Activity of Oxypeucedanin via Induction of G2/M Phase Cell Cycle Arrest and p53-Dependent MDM2/p21 Expression in Human Hepatoma Cells

Molecules ◽  
2020 ◽  
Vol 25 (3) ◽  
pp. 501
Author(s):  
So Hyun Park ◽  
Ji-Young Hong ◽  
Hyen Joo Park ◽  
Sang Kook Lee
Keyword(s):  
Cell Cycle ◽  
Cell Cycle Arrest ◽  
Cancer Cells ◽  
Antiproliferative Activity ◽  
Hepatoma Cells ◽  
Phase Cell ◽  
Human Hepatoma Cells ◽  
Cycle Arrest ◽  
Growth Inhibitory Activity ◽  
M Phase

Oxypeucedanin (OPD), a furocoumarin compound from Angelica dahurica (Umbelliferae), exhibits potential antiproliferative activities in human cancer cells. However, the underlying molecular mechanisms of OPD as an anticancer agent in human hepatocellular cancer cells have not been fully elucidated. Therefore, the present study investigated the antiproliferative effect of OPD in SK-Hep-1 human hepatoma cells. OPD effectively inhibited the growth of SK-Hep-1 cells. Flow cytometric analysis revealed that OPD was able to induce G2/M phase cell cycle arrest in cells. The G2/M phase cell cycle arrest by OPD was associated with the downregulation of the checkpoint proteins cyclin B1, cyclin E, cdc2, and cdc25c, and the up-regulation of p-chk1 (Ser345) expression. The growth-inhibitory activity of OPD against hepatoma cells was found to be p53-dependent. The p53-expressing cells (SK-Hep-1 and HepG2) were sensitive, but p53-null cells (Hep3B) were insensitive to the antiproliferative activity of OPD. OPD also activated the expression of p53, and thus leading to the induction of MDM2 and p21, which indicates that the antiproliferative activity of OPD is in part correlated with the modulation of p53 in cancer cells. In addition, the combination of OPD with gemcitabine showed synergistic growth-inhibitory activity in SK-Hep-1 cells. These findings suggest that the anti-proliferative activity of OPD may be highly associated with the induction of G2/M phase cell cycle arrest and upregulation of the p53/MDM2/p21 axis in SK-HEP-1 hepatoma cells.

scholarly journals Antiproliferative Activity and Potential Mechanism of Marine-Sourced Streptoglutarimide H against Lung Cancer Cells

Marine Drugs ◽  
2021 ◽  
Vol 19 (2) ◽  
pp. 79
Author(s):  
Hengju Ge ◽  
Di Zhang ◽  
Muran Shi ◽  
Xiaoyuan Lian ◽  
Zhizhen Zhang
Keyword(s):  
Lung Cancer ◽  
Cell Cycle ◽  
Cancer Cells ◽  
Antiproliferative Activity ◽  
Lung Cancer Cells ◽  
Potential Mechanism ◽  
Nucleotide Synthesis ◽  
Factor C ◽  
Antiglioma Activity

In 2019, streptoglutarimide H (SGH) was characterized as a new glutarimide from the secondary metabolites produced by a marine-derived actinomycete Streptomyces sp. ZZ741 and shown to have in vitro antiglioma activity. However, the antiproliferative activity and potential mechanism of SGH against lung cancer cells have not yet been characterized. This study demonstrated that SGH significantly inhibited the proliferation of different lung cancer cells. In terms of mechanism of action, SGH downregulated cell cycle- and nucleotide synthesis-related proteins to block cell cycle at G0/G1 phase, reduced the expression levels of glycolytic metabolic enzymes to inhibit glycolysis, and downregulated the important cancer transcription factor c-Myc and the therapeutic target deubiquitinase USP28. Potent anticancer activity and multiple mechanisms indicated SGH to be a novel antitumor compound against lung cancer cells.

scholarly journals Nicotinamide riboside–amino acid conjugates that are stable to purine nucleoside phosphorylase

2020 ◽  
Vol 18 (15) ◽  
pp. 2877-2885
Author(s):  
Faisal Hayat ◽  
Marie E. Migaud
Keyword(s):  
Amino Acid ◽  
Acid Ester ◽  
Purine Nucleoside Phosphorylase ◽  
Amino Acid Ester ◽  
Purine Nucleoside ◽  
Nucleoside Phosphorylase ◽  
Amino Acid Conjugates ◽  
Nicotinamide Riboside

O5′ amino acid ester conjugates of nicotinamide riboside, generated via a reduced intermediate, are stable to purine nucleoside phosphorylase.

Synthesis and anti-phlogistic potency of some new non-proteinogenic amino acid conjugates of ?Diclofenac?

Amino Acids ◽  
1999 ◽  
Vol 16 (3-4) ◽  
pp. 425-440 ◽  
Author(s):  
M. H. Abo-Ghalia ◽  
A. M. Shalaby ◽  
W. I. El-Eraqi ◽  
H. M. Awad
Keyword(s):  
Amino Acid ◽  
Amino Acid Conjugates ◽  
Proteinogenic Amino Acid

Synthesis and evaluation of some amino acid conjugates of pirprofen

2013 ◽  
Vol 3 (3) ◽  
pp. 241-246 ◽  
Author(s):  
S.K. Sharma ◽  
C. Karthikeyan ◽  
N.S. Hari Narayana Moorthy ◽  
D.K. Jain ◽  
P. Trivedi
Keyword(s):  
Amino Acid ◽  
Amino Acid Conjugates

An IMDAF approach to annellated 1,4:5,8-diepoxynaphthalenes and their metathesis reaction leading to novel scaffolds displaying an antiproliferative activity toward cancer cells

2021 ◽  
Author(s):  
Elizaveta A. Kvyatkovskaya ◽  
Kseniya K. Borisova ◽  
Polina P. Epifanova ◽  
Aleksey A. Senin ◽  
Victor N. Khrustalev ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Cell Lines ◽  
Cancer Cell ◽  
Antiproliferative Activity ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Metathesis Reaction ◽  
Human Cancer Cell Lines ◽  
Antiproliferative Agent

A 3,5a-epoxyfuro[2,3,4-de]isoquinoline scaffold, the product of ROCM of 1,4:5,8-diepoxynaphthalenes, is a promising antiproliferative agent toward breast and prostate human cancer cell lines.

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