scholarly journals Biological Evolution of Titanium(IV) Complex [{(NNO)2Ti}3O3] Bearing Bidentate Heteroditopic Schiff Base Ligand: Synthesis, Structure and Biological Studies

2019 ◽  
Vol 32 (2) ◽  
pp. 441-450
Author(s):  
Ravi K. Kottalanka ◽  
Eswar Pagadala ◽  
Shiva K. Loke ◽  
S. Rex Jeya Rajkumar ◽  
Venkatesan Srinivasadesikan ◽  
...  
Keyword(s):  
Schiff Base ◽  
Cell Lines ◽  
Cancer Cell ◽  
Biological Activities ◽  
Biological Significance ◽  
Cancer Cell Lines ◽  
Biologically Active ◽  
Binding Studies ◽  
Biological Studies

Titanium(IV)-complex of chemical composition [{(NNO)2Ti}3O3] (2) bearing bidentate heteroditopic Schiff base [(C5H4OH)-N=CH-C4H3-NH] (L1) ligand in titanium coordination sphere was reported and its biological significance was evaluated. The in vitro cytotoxicity of L1 and 2 were evaluated by using MTT assay on cancer cell lines (MCF-7 & A549) and observed significant cytotoxicity. Further, the LDH and NO assay studies on both L1 and 2 on cancer cell lines revealed that the enhanced cytotoxicity compared to standard anticancer drug i.e. cisplatin. The DNA binding studies of tested compounds with Ct-DNA molecule by using UV-visible and fluorescence spectra and molecular docking studies revealed that moderate to good binding interactions with test molecules. Thus, the present work contributes and implies the biological significance of Ti-complex (2) and the correlation between the structure and the biological activities of such Ti-complexes supported by Schiff base systems opens up opportunities for further exploitation of similar biologically active titanium systems.

scholarly journals Computational, Pharmacological and Toxicological Approach of Repurposed Lamotrigine Schiff Base Derivatives for Reduction of Hormone-Positive Breast Tumor

2021 ◽  
Author(s):  
Saima Najm ◽  
Humaira Naureen ◽  
Fareeha Anwar ◽  
Muhammad Mubbashir Khan ◽  
Rabia Ali
Keyword(s):  
Breast Cancer ◽  
Schiff Base ◽  
Cell Lines ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Cancer Cell Lines ◽  
Breast Cancer Cell Lines ◽  
Mcf 7

Abstract Background and objectives: Breast cancer presents high morbidity among women with various treatment challenges. This study aims to evaluate the repurposed lamotrigine schiff base metal (LTG-SB-M) coordinates against in-vitro MCF-7 breast cancer cell lines and in-vivo N-methylnitrosourea (NMU)-persuaded toxicity of rats’ mammary gland. Method: In-silico computational analysis and in vitro cytotoxic studies on MCF-7 breast cancer cell lines was executed to build up the assumptions. In-vivo NMU-induced anticancer potential was assessed in forty Wistar rats; assigned into five groups of 8 rats each. Group I served as normal control and received normal saline, Group II received NMU (50 mg/kg), Group III received tamoxifen, whereas; Group IV and V received LTG-SB-M derivative (LAC3, LBC3) at dose of 100 mg/kg body weight, for 15 consecutive days. Intraperitoneal injection of NMU (single dose) was given at the age of 5, 9 and 13 weeks to the rats with the three week interval. For all experimental animals; biochemical markers were assessed. DNA strand breakage alongside the hormonal profile of estrogen and progesterone was also estimated. Results: All tested compounds present significant activity against MCF-7 cell lines in vitro and NMU-induced mammary tumor in vivo. The in vivo results of tested compounds present a significant decrease in weight of organ; with reinstated renal and hepatic enzymes. Histological analysis revealed strong countenance of proteins, estrogen, and progesterone in NMU-treated rats. Conclusion: These results suggest that LTG-SB-M complex can be used as better anticancer agent against breast cancer.

New Approaches for the Synthesis of Heterocyclic Compounds Corporating benzo[d]imidazole as Anticancer Agents, Tyrosine, Pim-1 Kinases Inhibitions and their PAINS Evaluations

2020 ◽  
Vol 20 ◽  
Author(s):  
Rafat M. Mohareb ◽  
Yara R. Milad ◽  
Bahaa M. Mostafa ◽  
Reem A. El-Ansary
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Tyrosine Kinases ◽  
Heterocyclic Compounds ◽  
Cancer Cell Lines ◽  
Biologically Active ◽  
Strong Impact ◽  
Target Molecules

Background: Benzo[d]imidazoles are highly biologically active, in addition, they are considered as a class of heterocyclic compounds with many pharmaceutical applications. Objective: We are aiming in this work to synthesize target molecules not only possess anti-tumor activities but also kinase inhibitors. The target molecules were obtained starting from the benzo[d]imidazole derivatives followed by their heterocyclization reactions to produce anticancer target molecules. Methods: The 1-(1H-benzo[d]imidazol-2-yl)propan-2-one (3) and the ethyl 2-(1H-benzo[d]imidazol-2-yl)acetate (16) were used as the key starting material which reacted with salicylaldehyde to give the corresponding benzo[4,5]imidazo[1,2-a]quinoline derivatives. On the other hand, both of them were reacted with different reagents to give thiophene, pyran and benzo[4,5]imidazo[1,2-c]pyrimidine derivatives. The synthesized compounds were evaluated against the six cancer cell lines A549, HT-29, MKN-45, U87MG, and SMMC7721 and H460 together with inhibitions toward tyrosine kinases, c-Met kinase and prostate cancer cell line PC-3 were recorded using the standard MTT assay in vitro, with foretinib as the positive control. Results: Most of the synthesized compounds exhibited high inhibitions toward the tested cancer cell lines. In addition, tyrosine and Pim1 kinases inhibitions were performed for the most active compounds where variation of substituent through the aryl ring and heterocyclic ring afforded compounds with high activities. Our analysis showed that there is a strong correlation between structure of compound and substituents of target molecules. Conclusion: Our present research proved that the synthesized heterocyclic compounds with varieties of substituents has a strong impact through the activity of compounds. The evaluations through different cell lines and tyrosine kinases indicated that the compounds were excellent candidates as anticancer agents. This could encourage doing further research within this field for the building of compounds with high inhibitions.

scholarly journals Synthesis, Antiproliferative Activity, and DNA Binding Studies of Nucleoamino Acid-Containing Pt(II) Complexes

2020 ◽  
Vol 13 (10) ◽  
pp. 284
Author(s):  
Claudia Riccardi ◽  
Domenica Capasso ◽  
Angela Coppola ◽  
Chiara Platella ◽  
Daniela Montesarchio ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Synergistic Effects ◽  
Polyacrylamide Gel Electrophoresis ◽  
Platinum Complexes ◽  
Cancer Cell Lines ◽  
Cd Spectroscopy ◽  
Model Systems ◽  
Binding Studies

We here report our studies on the reaction with the platinum(II) ion of a nucleoamino acid constituted by the l-2,3-diaminopropanoic acid linked to the thymine nucleobase through a methylenecarbonyl linker. The obtained new platinum complexes, characterized by spectroscopic and mass spectrometric techniques, were envisaged to exploit synergistic effects due to the presence of both the platinum center and the nucleoamino acid moiety. The latter can be potentially useful to protect the complexes from early deactivation, as well as to facilitate their cell internalization. The biological activity of the complexes in terms of antiproliferative effects was evaluated in vitro on different cancer cell lines and healthy cells, showing the best results on human cervical adenocarcinoma (HeLa) cells along with good selectivity for cancer over normal cells. In contrast, the metal-free nucleoamino acid did not show any cytotoxicity on both normal and cancer cell lines. Finally, the ability of the novel Pt(II) complexes to bind various DNA model systems was investigated by circular dichroism (CD) spectroscopy and polyacrylamide gel electrophoresis analyses proving that the newly obtained compounds can potentially target DNA, similarly to other well-known anticancer Pt complexes, with a peculiar G-quadruplex vs. duplex selectivity.

scholarly journals Design, Synthesis, and Antipoliferative Activities of Novel Substituted Imidazole-Thione Linked Benzotriazole Derivatives

Molecules ◽  
2021 ◽  
Vol 26 (19) ◽  
pp. 5983
Author(s):  
Ahdab N. Khayyat ◽  
Khaled O. Mohamed ◽  
Azizah M. Malebari ◽  
Afaf El-Malah
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Tubulin Polymerization ◽  
Design Synthesis ◽  
Biological Studies ◽  
Phase Compound ◽  
Hct 116 ◽  
Mcf 7

A new series of benzotriazole moiety bearing substituted imidazol-2-thiones at N1 has been designed, synthesized and evaluated for in vitro anticancer activity against the different cancer cell lines MCF-7(breast cancer), HL-60 (Human promyelocytic leukemia), and HCT-116 (colon cancer). Most of the benzotriazole analogues exhibited promising antiproliferative activity against tested cancer cell lines. Among all the synthesized compounds, BI9 showed potent activity against the cancer cell lines such as MCF-7, HL-60 and HCT-116 with IC50 3.57, 0.40 and 2.63 µM, respectively. Compound BI9 was taken up for elaborate biological studies and the HL-60 cells in the cell cycle were arrested in G2/M phase. Compound BI9 showed remarkable inhibition of tubulin polymerization with the colchicine binding site of tubulin. In addition, compound BI9 promoted apoptosis by regulating the expression of pro-apoptotic protein BAX and anti-apoptotic proteins Bcl-2. These results provide guidance for further rational development of potent tubulin polymerization inhibitors for the treatment of cancer.

Lawsone (2-hydroxy-1,4-naphthaquinone) derived anticancer agents

2022 ◽  
Vol 0 (0) ◽  
Author(s):  
Arvind Singh ◽  
Amartya Basu ◽  
Aditi Sharma ◽  
Anu Priya ◽  
Manmmet Kaur ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Biological Activities ◽  
Cancer Cell Lines ◽  
Biologically Active ◽  
Synthetic Methods ◽  
Lawsonia Inermis ◽  
Wide Range ◽  
Tree Leaf

Abstract 2-Hydroxy-1,4-naphthaquinone, commonly known as lawsone, represents an extremely important biologically active naturally occurring compound. It can easily be isolated from Lawsonia inermis (henna) tree leaf extract. Last decade has seen tremendous applications of lawsone as a starting component for the preparation of various organic scaffolds. Many of these synthesized scaffolds showed a wide range of biological activities including potential activities towards several cancer cell lines. This review deals with diverse synthetic methods of lawsone derived scaffolds and their screening against different anti-cancer cell lines along with promising results.

scholarly journals Design, Synthesis and Anticancer activity of novel Triazole substituted Quinazoline Hybrids

2020 ◽  
Vol 11 (3) ◽  
pp. 3569-3579
Author(s):  
Paduri Karunakar ◽  
Swetha Gujjewar ◽  
Somesh Sharma ◽  
Srinivasu Pothukanuri ◽  
Krubakaran Muthusamy ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Biological Activities ◽  
Cancer Cell Line ◽  
Cancer Cell Lines ◽  
Breast Cancer Cell Lines ◽  
Liver Carcinoma ◽  
Synthetic Approach

Quinazolines and 1,2,4-triazoles are important class of nitrogen containing heterocyclic compounds having immense biological importance. From the literature review, pharmacokinetic properties of a drug can be modified or enhanced by building a triazole moiety into a compound like quinazoline. Therefore, the study of new hybrid systems which combines triazole system with quinazoline is still seemed warranted. In the present study, a sequence of novel 1,2,4-triazole derivatives containing quinazolinyl moiety were designed, synthesized and screened for their in vitro anticancer activity. Thirteen new hybrids are synthesized from readily accessible 5-bromoanthranilic acid. All the hybrid compounds were well explicated by IR, 1H, 13C NMR, and mass spectral data. Out of 13, some of the compounds manifested moderate to good antiproliferative activity against two cancer cell lines (HepG2 and MCF7). Remarkably, compounds 8A, 16H and 16K displayed potent activity (14- 49 µM) on both HepG2 (liver carcinoma) and MCF-7 (breast cancer) cell lines whereas compounds 8B, 8F, 16L, and 15 displayed substantial activity against HepG2 cancer cell line (34-65 µM). Synthetic approach described here is very simple and can be used for the syntheses of related compounds library which is useful for the exploration of further biological activities and is currently underway in our laboratory

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