scholarly journals Amino Acids and Peptides as Versatile Ligands in the Synthesis of Antiproliferative Gold Complexes

Chemistry ◽  
2020 ◽  
Vol 2 (2) ◽  
pp. 203-218 ◽  
Author(s):  
Tina P. Andrejević ◽  
Biljana Đ. Glišić ◽  
Miloš I. Djuran
Keyword(s):  
Rheumatoid Arthritis ◽  
Amino Acids ◽  
Future Development ◽  
Antitumor Agents ◽  
Review Article ◽  
Gold Complexes ◽  
Different Types ◽  
Potential Antitumor

Gold complexes have been traditionally employed in medicine, and currently, some gold(I) complexes, such as auranofin, are clinically used in the treatment of rheumatoid arthritis. In the last decades, both gold(I) and gold(III) complexes with different types of ligands have gained considerable attention as potential antitumor agents, showing superior activity both in vitro and in vivo to some of the clinically used agents. The present review article summarizes the results achieved in the field of synthesis and evaluation of gold complexes with amino acids and peptides moieties for their cytotoxicity. The first section provides an overview of the gold(I) complexes with amino acids and peptides, which have shown antiproliferative activity, while the second part is focused on the activity of gold(III) complexes with these ligands. A systematic summary of the results achieved in the field of gold(I/III) complexes with amino acids and peptides could contribute to the future development of metal complexes with these biocompatible ligands as promising antitumor agents.

Synthesis and biological evaluation of novel bivalent β-carbolines as potential antitumor agents

MedChemComm ◽  
2014 ◽  
Vol 5 (7) ◽  
pp. 953-957 ◽  
Author(s):  
Qifeng Wu ◽  
Zhushuang Bai ◽  
Qin Ma ◽  
Wenxi Fan ◽  
Liang Guo ◽  
...  
Keyword(s):  
Antitumor Agents ◽  
Biological Evaluation ◽  
Cytotoxic Activities ◽  
Lewis Lung ◽  
Lewis Lung Cancer ◽  
Synthesis And Biological Evaluation ◽  
Tumor Inhibition Rate ◽  
Potential Antitumor

A series of bivalent β-carbolines with a spacer between the 3-carboxyl oxygens was synthesized and their cytotoxic activities in vitro and antitumor efficacies in vivo were evaluated. Compound 22 exhibited potent antitumor activity against Lewis lung cancer in mice with a tumor inhibition rate of 64.2%.

Strong In Vitro And Vivo Cytotoxicity Of Two Platinum(II) Complexes With Cryptolepine Derivatives

2021 ◽  
Author(s):  
Li-Qin Qin ◽  
Zu-Zhuang Wei ◽  
Lin Yang ◽  
Qi-Pin Qin ◽  
Jia-Jing Zeng ◽  
...  
Keyword(s):  
Mitochondrial Dysfunction ◽  
Cancer Cells ◽  
Cell Apoptosis ◽  
Antitumor Agents ◽  
Cytotoxic Activities ◽  
Antitumor Activities ◽  
Branched Chain ◽  
Potential Antitumor

Abstract Two mononuclear Pt(II) compounds, [Pt(BQL1)Cl]Cl (BQL1-Pt) and [Pt(BQL2)Cl]Cl (BQL2-Pt) with [5-(benzo[4,5]furo[3,2-b]quinolin-11-yloxy)-pentyl]-bis-pyridin-2-ylmethyl-amine (BQL1) and [9-(benzo[4,5]furo[3,2-b]quinolin-11-yloxy)-nonyl]-bis-pyridin-2-ylmethyl-amine (BQL2), were prepared as new chemotypes for potential antitumor agents. This study evaluated the influence of cryptolepine derivatives in BQL1-Pt, 2,2′-dipicolylamine Pt(II) complex, and BQL2-Pt on cellular Pt(II) accumulation, cytotoxicity, and in vitro and in vivo antitumor activities against T-24 cancer cells and normal HL-7702 cells. BQL1-Pt and BQL2-Pt displayed cytotoxic activities in the micromole range (1.3±0.1 and 0.2±0.2 μM, respectively) on T-24 cancer cells; however, they did not exhibit any toxicity against HL-7702 cells. They triggered T-24 cell apoptosis through a mitochondrial dysfunction pathway. Compared to 2,2′-dipicolylamine, the neutral BQL1 and BQL2 ligands with cryptolepine derivatives increased the planarity and branched chain resulting in BQL1-Pt and BQL2-Pt with favorable antitumor activities. Further, BQL2-Pt effectively inhibited the growth of bladder T-24 tumor in vivo. BQL2-Pt can act as a potential therapeutic candidate for cancer treatment.

Stilbenes and Xanthones from Medicinal Plants as Potential Antitumor Agents

2020 ◽  
Vol 16 ◽  
Author(s):  
Eugenia Dumitra Teodor ◽  
Oana Ungureanu ◽  
Veronica Moroeanu ◽  
Gabriel Lucian Radu
Keyword(s):  
Medicinal Plants ◽  
Anticancer Agents ◽  
Antitumor Agents ◽  
Plant Polyphenols ◽  
Natural Substances ◽  
Abnormal Cells ◽  
Digestive Disorders ◽  
Potential Antitumor

Abstract:: There is an emerging interest for plant polyphenols as dietary ingredients, particularly in digestive disorders and/or as antitumor agents. The plant compounds or extracts continue to be an alternative to drug use, many studies being aimed to find natural substances with selective cytotoxicity on abnormal cells. Phenolic compounds as important secondary metabolites from plants are intensively studied as substitute of drugs. In this review, the recent literature data from past five years about potential anticancer/antitumor effect of some categories of phenolics such as stilbenes and xanthones extracted from medicinal plants are surveyed. The most important results concerning the effectiveness as antitumor/anticancer agents of these active compounds, as isolated compounds or as plant extracts, some bioavailability aspects and their mechanism of action in vitro and in vivo were considered.

scholarly journals Synthesis and Biological Evaluation of Novel 4-(4-Formamidophenylamino)-N-methylpicolinamide Derivatives as Potential Antitumor Agents

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 1150
Author(s):  
Nana Meng ◽  
Shuyan Zhou ◽  
Min Hu ◽  
Youzhi Xu ◽  
Yong Xia ◽  
...  
Keyword(s):  
Cell Lines ◽  
Antitumor Agents ◽  
Human Cancer ◽  
Biological Evaluation ◽  
Human Cancer Cell Lines ◽  
Apoptosis And Necrosis ◽  
Synthesis And Biological Evaluation ◽  
Potential Antitumor

A novel series of 4-(4-formamidophenylamino)-N-methylpicolinamide derivatives were synthesized and evaluated against different tumor cell lines. Experiments in vitro showed that these derivatives could inhibit the proliferation of two kinds of human cancer cell lines (HepG2, HCT116) at low micromolar concentrations and the most potent analog 5q possessed broad-spectrum antiproliferative activity. Experiments in vivo demonstrated that 5q could effectively prolong the longevity of colon carcinoma-burdened mice and slow down the progression of cancer cells by suppression of angiogenesis and the induction of apoptosis and necrosis.

Vitamin D as potential therapeutic anticancer agent

2018 ◽  
pp. 1-3
Keyword(s):  
Vitamin D ◽  
Anticancer Activity ◽  
Anticancer Agent ◽  
Antitumor Agents ◽  
Metastatic Potential ◽  
Anticancer Properties ◽  
Chemotherapy Agents

The role of vitamin D is implicated in carcinogenesis through numerous biological processes like induction of apoptosis, modulation of immune system inhibition of inflammation and cell proliferation and promotion of cell differentiation. Its use as additional adjuvant drug with cancer treatment may be novel combination for improved outcome of different cancers. Numerous preclinical, epidemiological and clinical studies support the role of vitamin D as an anticancer agent. Anticancer properties of vitamin D have been studied widely (both in vivo and in vitro) among various cancers and found to have promising results. There are considerable data that indicate synergistic potential of calcitriol and antitumor agents. Possible mechanisms for modulatory anticancer activity of vitamin D include its antiproliferative, prodifferentiating, and anti-angiogenic and apoptic properties. Calcitriol reduces invasiveness and metastatic potential of many cancer cells by inhibiting angiogenesis and regulating expression of the key molecules involved in invasion and metastasis. Anticancer activity of vitamin D is synergistic or additive with the antineoplastic actions of several drugs including cytotoxic chemotherapy agents like paclitaxel, docetaxel, platinum base compounds and mitoxantrone. Benefits of addition of vitamin D should be weighed against the risk of its toxicity.

Comparison of In Vitro and In Vivo Effects of Infliximab on Cytokine Production in Proliferating CD4+ T Cells in Patients with Rheumatoid Arthritis

2015 ◽  
Vol 1 (2) ◽  
pp. 122-128
Author(s):  
Syuichi Koarada ◽  
Yuri Sadanaga ◽  
Natsumi Nagao ◽  
Satoko Tashiro ◽  
Rie Suematsu ◽  
...  
Keyword(s):  
Rheumatoid Arthritis ◽  
T Cells ◽  
Cd4 T Cells ◽  
Cytokine Production

The 1- and 2-Naphthylalanine Analogs of Oxytocin and Vasopressin

1995 ◽  
Vol 60 (12) ◽  
pp. 2170-2177 ◽  
Author(s):  
Zdenko Procházka ◽  
Jiřina Slaninová
Keyword(s):  
Amino Acids ◽  
Solid Phase ◽  
Pressor Test

Solid phase technique on p-methylbenzhydrylamine resin was used for the synthesis of four analogs of oxytocin and four analogs of vasopressin with the non-coded amino acids L- or D- and 1- or 2-naphthylalanine and D-homoarginine. [L-1-Nal2]oxytocin, [D-1-Nal2]oxytocin, [L-2-Nal2]oxytocin, [D-2-Nal2]oxytocin, [L-1-Nal2, D-Har8]vasopressin, [D-1-Nal2, D-Har8]vasopressin, [L-2-Nal2, D-Har8]vasopressin and [D-2-Nal2, D-Har8]vasopressin were synthesized. All eight analogs were found to be uterotonic inhibitors in vitro and in vivo. Analogs with 2-naphthylalanine are stronger inhibitors, particularly in the vasopressin series than the analogs with 1-naphthylalanine. Analogs with 1-naphthylalanine have no activity in the pressor test, analogs with 2-naphthylalanine are weak pressor inhibitors.

scholarly journals Design, Synthesis, Molecular Modeling and Antitumor Evaluation of Novel Indolyl-Pyrimidine Derivatives with EGFR Inhibitory Activity

Molecules ◽  
2021 ◽  
Vol 26 (7) ◽  
pp. 1838
Author(s):  
Naglaa M. Ahmed ◽  
Mahmoud M. Youns ◽  
Moustafa K. Soltan ◽  
Ahmed M. Said
Keyword(s):  
Molecular Modeling ◽  
Antitumor Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Antiproliferative Activity ◽  
Antitumor Agents ◽  
Cancer Cell Lines ◽  
Normal Cells

Scaffolds hybridization is a well-known drug design strategy for antitumor agents. Herein, series of novel indolyl-pyrimidine hybrids were synthesized and evaluated in vitro and in vivo for their antitumor activity. The in vitro antiproliferative activity of all compounds was obtained against MCF-7, HepG2, and HCT-116 cancer cell lines, as well as against WI38 normal cells using the resazurin assay. Compounds 1–4 showed broad spectrum cytotoxic activity against all these cancer cell lines compared to normal cells. Compound 4g showed potent antiproliferative activity against these cell lines (IC50 = 5.1, 5.02, and 6.6 μM, respectively) comparable to the standard treatment (5-FU and erlotinib). In addition, the most promising group of compounds was further evaluated for their in vivo antitumor efficacy against EAC tumor bearing mice. Notably, compound 4g showed the most potent in vivo antitumor activity. The most active compounds were evaluated for their EGFR inhibitory (range 53–79 %) activity. Compound 4g was found to be the most active compound against EGFR (IC50 = 0.25 µM) showing equipotency as the reference treatment (erlotinib). Molecular modeling study was performed on compound 4g revealed a proper binding of this compound inside the EGFR active site comparable to erlotinib. The data suggest that compound 4g could be used as a potential anticancer agent.

scholarly journals Secreted KIAA1199 promotes the progression of rheumatoid arthritis by mediating hyaluronic acid degradation in an ANXA1-dependent manner

2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Wei Zhang ◽  
Guoyu Yin ◽  
Heping Zhao ◽  
Hanzhi Ling ◽  
Zhen Xie ◽  
...  
Keyword(s):  
Rheumatoid Arthritis ◽  
Hyaluronic Acid ◽  
Dependent Manner ◽  
Collagen Induced Arthritis ◽  
Intracellular Degradation ◽  
Main Pathway ◽  
First Time

AbstractIn inflamed joints, enhanced hyaluronic acid (HA) degradation is closely related to the pathogenesis of rheumatoid arthritis (RA). KIAA1199 has been identified as a hyaladherin that mediates the intracellular degradation of HA, but its extracellular function remains unclear. In this study, we found that the serum and synovial levels of secreted KIAA1199 (sKIAA1199) and low-molecular-weight HA (LMW-HA, MW < 100 kDa) in RA patients were significantly increased, and the positive correlation between them was shown for the first time. Of note, treatment with anti-KIAA1199 mAb effectively alleviated the severity of arthritis and reduced serum LMW-HA levels and cytokine secretion in collagen-induced arthritis (CIA) mice. In vitro, sKIAA1199 was shown to mediate exogenous HA degradation by attaching to the cell membrane of RA fibroblast-like synoviosytes (RA FLS). Furthermore, the HA-degrading activity of sKIAA1199 depended largely on its adhesion to the membrane, which was achieved by its G8 domain binding to ANXA1. In vivo, kiaa1199-KO mice exhibited greater resistance to collagen-induced arthritis. Interestingly, this resistance could be partially reversed by intra-articular injection of vectors encoding full-length KIAA1199 instead of G8-deleted KIAA119 mutant, which further confirmed the indispensable role of G8 domain in KIAA1199 involvement in RA pathological processes. Mechanically, the activation of NF-κB by interleukin-6 (IL-6) through PI3K/Akt signaling is suggested to be the main pathway to induce KIAA1199 expression in RA FLS. In conclusion, our study supported the contribution of sKIAA1199 to RA pathogenesis, providing a new therapeutic target for RA by blocking sKIAA1199-mediated HA degradation.

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