C , O ‐Chelated organotin(IV) derivatives as potential anticancer agents: Synthesis, characterization, and cytotoxic activity

2022 ◽  
Author(s):  
Adrian‐Alexandru Someșan ◽  
Sabina‐Mădălina Vieriu ◽  
Alexandru Crăciun ◽  
Cristian Silvestru ◽  
Paul Chiroi ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Anticancer Agents

scholarly journals Synthesis and Cytotoxic Analysis of Novel Myrtenyl Grafted Pseudo-Peptides Revealed Potential Candidates for Anticancer Therapy

Molecules ◽  
2020 ◽  
Vol 25 (8) ◽  
pp. 1911 ◽  
Author(s):  
Odette Concepción ◽  
Julio Belmar ◽  
Alexander F. de la Torre ◽  
Francisco M. Muñiz ◽  
Mariano W. Pertino ◽  
...  
Keyword(s):  
T Cells ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Cd4 T Cells ◽  
Dermal Fibroblast ◽  
Colon Adenocarcinoma ◽  
Cancer Cell Lines ◽  
Biological Properties

Myrtenal is a natural monoterpene isolated from essential oils of several plants and their derivates have shown to have several biological properties including cytotoxicity. The cytotoxic activity of these derivates are being investigated for their antitumor effect leading to the development of potential anticancer agents. In this study, novels Myrtenyl grafted pseudo-peptides were designed, synthesized and functionally characterized as possible therapeutic agents for cancer treatment. Thirteen novel Myrtenyl grafted pseudo-peptides were prepared in high atom economy and efficiency by a classic Ugi-4CR and sequential post-modification. Their structures were confirmed by NMR, and ESI-MS, and its cytotoxic activity was evaluated in three cancer cell lines and primary CD4+ T cells at different proliferative cycles. Our results revealed that some of these compounds showed significant cytotoxicity against human gastric, breast and colon adenocarcinoma cells lines, but not against human dermal fibroblast cell line. Moreover, from the thirteen novel myrtenyl synthesized the compound (1R,5S)-N-{[1-(3-chlorophenyl)-1H-1,2,3-triazol-4-yl]methyl}-N-[2-(cyclohexylamino)-2–oxoethyl]-6,6-dimethylbicyclo[3.1.1]hept-2-ene-2-carboxamide (3b) proved to be the best candidate in terms of acceptable EC50, and Emax values in cancer cell lines and at inducing cytotoxicity in CD4+ T cells undergoing active proliferation, without affecting non-proliferating T cells. Overall, the synthesis and characterization of our Myrtenyl derivates revealed novel potential anticancer candidates with selective cytotoxic activity.

Synthesis, cytotoxic activity, and 2D- and 3D-QSAR studies of 19-carboxyl-modified novel isosteviol derivatives as potential anticancer agents

2017 ◽  
Vol 89 (6) ◽  
pp. 870-887 ◽  
Author(s):  
Cong-Jun Liu ◽  
Tao Zhang ◽  
Shu-Ling Yu ◽  
Xing-Jie Dai ◽  
Ya Wu ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Anticancer Agents ◽  
3D Qsar ◽  
Qsar Studies ◽  
2D And 3D

scholarly journals The cytotoxic activity of pine needles ethanolic extract of Pinus merkusii on HeLa cell lines

2021 ◽  
Vol 33 ◽  
pp. 03001
Author(s):  
Annise Proboningrat ◽  
Amaq Fadholly ◽  
Sri Agus Sudjarwo ◽  
Fedik Abdul Rantam ◽  
Agung Budianto Achmad
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Anticancer Agent ◽  
Ethanolic Extract ◽  
In Vitro Cytotoxicity ◽  
Hela Cell Lines ◽  
Cytotoxicity Assessment ◽  
Pinus Merkusii

Several efforts have been made to discover new anticancer agents based on natural ingredients. Meanwhile, previous studies have shown that different Pine genus species exhibit cytotoxic activity against various types of cancer cells. This plant is rich in phenolic compounds, especially procyanidins, flavonoids, and phenolic acids. Therefore, this study aims to investigate the in vitro cytotoxicity of Pinus merkusii needles extract on HeLa cancer cell lines. The cytotoxicity assessment was measured using MTT assay and expressed as IC50 value. The results showed that the ethanolic extract poses a dose and time-dependent cytotoxic activity with an IC50 value of 542.5 µg/ml at 48 hours of incubation. Based on this result, Pinus merkusii needles’ ethanolic extract has the potential of a novel candidate for an anticancer agent.

Synthesis and evaluation of new benzimidazole derivatives with hydrazone moiety as anticancer agents

2018 ◽  
Vol 43 (2) ◽  
pp. 151-158 ◽  
Author(s):  
Ulviye Acar Çevik ◽  
Begüm Nurpelin Sağlık ◽  
Cankız Mina Ardıç ◽  
Yusuf Özkay ◽  
Özlem Atlı
Keyword(s):  
Cytotoxic Activity ◽  
Anticancer Agents ◽  
Point Of View ◽  
Current Therapy ◽  
Benzimidazole Derivatives ◽  
Anticancer Activities ◽  
New Chemical Entities ◽  
Nih 3T3 ◽  
Mcf 7

Abstract Objectives: Cancer is one of the leading causes of death throughout the world. Current therapy options suffer from the major limitations of side effects and drug resistance. Thus, continuing search for newer and safer anticancer drugs remains critically important. From this point of view, in the present study benzimidazole-hydrazone derivatives were synthesized by aiming at the identification of new chemical entities as potent anticancer agents. Material and methods: A series of 12 new compounds of 4-(5(6)-substituted-1H-benzimidazol-2-yl)-N′thiophen/furan-2-yl-methylene) benzohydrazide derivatives were synthesized. The structures of the obtained compounds were elucidated using by IR, 1H NMR, 13C NMR, mass spectroscopy and elemental analyses. In vitro cytotoxic activity of the compounds against A549, MCF-7 and NIH/3T3 cell lines was evaluated by MTT assay. Results: Among the tested compounds, compound 3e showed higher cytotoxicity against MCF-7 human breast cancer cells when compared with cisplatin. Also, it has lower cytotoxicty against healthy cell line, NIH/3T3. Conclusions: It was determined that compound 3e showed inhibition towards MCF-7. Considering the substituent effect on cytotoxic activity, compound 3e bearing 2-methylthiophene has attracted attention with its higher anticancer activities.

Terpyridine Copper(II) Complexes as Potential Anticancer Agents by Inhibiting Cell Proliferation, Blocking Cell Cycle and Inducing Apoptosis in BEL-7402 Cells

2022 ◽  
Author(s):  
Yunqiong Gu ◽  
Yu-Jun Zhong ◽  
Mei-Qi Hu ◽  
Huan-Qing Li ◽  
Kun Yang ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Cell Proliferation ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Cancer Cell Lines

Four mononuclear terpyridine complexes [Cu(H-La)Cl2]·CH3OH (1), [Cu(H-La)Cl]ClO4 (2), [Cu(H-Lb)Cl2]·CH3OH (3), and [Cu(H-Lb)(CH3OH)(DMSO)](ClO4)2 (4) were prepared and fully characterized. Complexes 14 exhibited higher cytotoxic activity against several tested cancer cell lines...

scholarly journals Synthesis, characterization, antimicrobial screening and cytotoxic properties of Cu(II) and Zn(II) complexes with bidentate hydroxylated 1,3-diaryl-2-propene-1-ones ligand

2020 ◽  
pp. 68-68
Author(s):  
Pravinkumar Patil ◽  
Sainath Zangade
Keyword(s):  
Antimicrobial Activity ◽  
Metal Complexes ◽  
Cytotoxic Activity ◽  
Anticancer Agents ◽  
Cancer Cell Line ◽  
Artemia Salina ◽  
Carbonyl Oxygen ◽  
Planar Geometry ◽  
Ft Ir

A series of binary metal complexes [halo, hydroxyl and methoxy sub-stituted bis (2-(E) acryloyl)naphthalen-1-yl)oxy)Cu(II) and Zn(II) (C1-C10)] of Cu2+ and Zn2+ ions derived from bi-coordinated hydroxylated 1,3-diaryl-2- -propene-1-ones were synthesized. The newly synthesized metal complexes were structurally determined by FT-IR, 1H NMR, 13CNMR, ESR spectral, XRD and TGA analysis. The FT-IR and ESR studies demonstrated that interactions between metal ions with ligands occur through carbonyl oxygen and deprotonated hydroxyl oxygen and corresponds to square-planar geometry for all complexes. In-vitro the metal complexes were screened and evaluated for their antimicrobial and cytotoxic activity. The complexes C1 and C4 showed the significant antimicrobial activity while the remaining complexes were showed the moderately antimicrobial activity against the tested pathogens. The complexes were evaluated for cytotoxic activity against the organism Artemia salina. The complexes C2, C3, C4 and C5 were showed the LC50 values as 630.45, 969.99, 921.94 and 918.41 ?M mL-1 respectively. Further complexes were evaluated for anticancer activity against liver cancer cell line (Hep G2) in comparison with 5-fluorouracil standard. The complex C5 showed the significant IC50 value 58.94 ?g mL-1. Therefore the present study is useful to develop the new class of antimicrobial and anticancer agents.

scholarly journals A REVIEW ON CYTOTOXIC ACTIVITY OF (GARCINIA COWA ROXB.): POTENTIAL AS AN ANTICANCER

2020 ◽  
Vol 11 (12) ◽  
pp. 1-6
Author(s):  
Nur Syakila ◽  
Aried Eriadi ◽  
Dwi Dinni Aulia Bakhtra ◽  
Ridho Asra
Keyword(s):  
Cancer Therapy ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Death Rate ◽  
Prevention And Treatment ◽  
Cytotoxic Compounds ◽  
Garcinia Cowa ◽  
Made In

Cancer is a disease of abnormal body tissue cells that turn malignant. From the data, it can be seen that new cases and the death rate from cancer continues to increase every year so that efforts are made in the search for new anticancer agents for the prevention and treatment of cancer. There are many natural ingredients that can be used for its benefits, one of which is the Asam Kandis plant (Garcinia cowa Roxb.) This plant is rich in phytochemicals. It can be an important source of natural cytotoxic compounds and has potential as an anticancer. The analysis showed that the extract or compound from the roots, bark, twigs, leaves, and fruit rind of Asam Kandis (Garcinia cowa Roxb.) has good cytotoxic activity and is active against cancer cell lines so that it can help in the development of cancer therapy.

scholarly journals Anti-proliferative Activity of Some Oleanolic Acid Derivatives with Potent Topoisomerase Inhibitory Activity on B16 Melanoma Cells

2020 ◽  
Vol 9 (1) ◽  
pp. 26-28
Author(s):  
Ahmed Ashour ◽  
Ryuichiro Kondo ◽  
Kuniyoshi Shimizu
Keyword(s):  
Cytotoxic Activity ◽  
Oleanolic Acid ◽  
Anticancer Agents ◽  
Inhibitory Activity ◽  
Topoisomerase I ◽  
Melanoma Cells ◽  
Docking Studies ◽  
B16 Melanoma ◽  
Melanoma Cancer ◽  
B16 Melanoma Cells

Our previous study included the semisynthetic reactions on oleanolic acid, a common wood-derived oleanane-type triterpene. Ten rationally designed derivatives of oleanolic acid were synthesized based on docking studies and tested for their topoisomerase I and IIα inhibitory activity. Semisynthetic reactions targeted C-3, C-12, C-13 and C-17. Some of these compounds act as dual inhibitors for both topoisomerase I and IIα giving new anticancer agents. The cytotoxic activity of these compounds on B16 melanoma cancer cells was evaluated. Results showed that most of these compounds have a higher cytotoxic activity on B16 melanoma cells.

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