scholarly journals Design, Synthesis, and Structural Characterization of Novel Diazaphenothiazines with 1,2,3-Triazole Substituents as Promising Antiproliferative Agents

Molecules ◽  
2019 ◽  
Vol 24 (23) ◽  
pp. 4388 ◽  
Author(s):  
Morak-Młodawska ◽  
Pluta ◽  
Latocha ◽  
Jeleń ◽  
Kuśmierz
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Human Fibroblasts ◽  
Human Tumor ◽  
Design Synthesis ◽  
Human Tumor Cell Lines ◽  
Ic50 Values ◽  
Normal Human ◽  
Low Cytotoxicity

A series of novel 1,2,3-triazole-diazphenothiazine hybrids was designed, synthesized, and evaluated for anticancer activity against four selected human tumor cell lines (SNB-19, Caco-2, A549, and MDA-MB231). The majority of the synthesized compounds exhibited significant potent activity against the investigated cell lines. Among them, compounds 1d and 4c showed excellent broad spectrum anticancer activity, with IC50 values ranging from 0.25 to 4.66 μM and 0.25 to 6.25 μM, respectively. The most promising compound 1d, possessing low cytotoxicity against normal human fibroblasts NHFF, was used for gene expression analysis using reverse transcription–quantitative real-time PCR (RT–qPCR). The expression of H3, TP53, CDKN1A, BCL-2, and BAX genes revealed that these compounds inhibited the proliferation in all cells (H3) and activated mitochondrial events of apoptosis (BAX/BCL-2).

scholarly journals Design, Synthesis, and Anticancer Evaluation of Fused 1,2-diazine Derivatives

Proceedings ◽  
2019 ◽  
Vol 22 (1) ◽  
pp. 26
Author(s):  
Vasilichia ◽  
Dorina ◽  
Violeta ◽  
Ramona ◽  
Ionel
Keyword(s):  
Breast Cancer ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Human Tumor ◽  
Design Synthesis ◽  
Standard Drug ◽  
Human Tumor Cell Lines ◽  
20 Nm ◽  
Effective Drugs

Cancer is one of the most serious and merciless health problems of humankind, and the number of new cases is expected to increase in the next decades. Despite extensive cancer research in order to find more effective drugs and treatments, cancer chemotherapy is complex and complicated, because of the limited efficacy of drugs, significant levels of toxicity, and lack of selectivity, and the emergence of drug resistance and multidrug resistance make the situation even worse. We report here the design, synthesis, structure, and in vitro anticancer activity of two series of compounds derived from pyridazine and phthalazine. The in vitro anticancer activity was tested on a panel of 60 human tumor cell lines representing cancers of the brain, breast, colon, kidney, lung, ovary, prostate, as well as leukemia and melanoma, to the National Cancer Institute (USA). The test was conducted on a single dose and five dose assay. Notably, from the tested compounds, five of them show very good anticancer activity (superior to Doxorubicin, the NCI standard drug for this type of analysis), with a growth inhibition in the area of nanomolar, between 20–100 nM, on several cancer cell lines: breast cancer MCF7, colon cancer HCT-15, KM12 and SW-620, leukemia K562 and SR, melanoma MDA-MB-435, SK-MEL-5, and UACC-62, and renal cancer A498. SAR correlation in the two series and in between the two series has been performed. One compound has an excellent anticancer activity against breast cancer MCF7 cell, leukemia SR cell, and melanoma MDA-MB-435 cell, in the area of 20 nM.

scholarly journals Anticancer activity of pyrimidodiazepines based on 2-chloro-4-anilinoquinazoline: synthesis, DNA binding and molecular docking

RSC Advances ◽  
2021 ◽  
Vol 11 (38) ◽  
pp. 23310-23329
Author(s):  
Viviana Cuartas ◽  
Alberto Aragón-Muriel ◽  
Yamil Liscano ◽  
Dorian Polo-Cerón ◽  
Maria del Pilar Crespo-Ortiz ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Dna Binding ◽  
Tumor Cell ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Human Tumor ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines

A new series of quinazoline-based chalcones and pyrimidodiazepines were tested against 60 human tumor cell lines.

scholarly journals Labdane and Abietane Diterpenoids from Juniperus oblonga and Their Cytotoxic Activity

Molecules ◽  
2019 ◽  
Vol 24 (8) ◽  
pp. 1561 ◽  
Author(s):  
Qiao ◽  
Khutsishvili ◽  
Alizade ◽  
Atha ◽  
Borris
Keyword(s):  
Cell Lines ◽  
Human Tumor ◽  
2D Nmr ◽  
Human Tumor Cell Lines ◽  
Abietane Diterpenoids ◽  
Whole Plant ◽  
Phytochemical Investigation ◽  
Ic50 Values ◽  
First Time ◽  
Mcf 7

A phytochemical investigation of the whole plant of Juniperus oblonga led to the isolationof one previously undescribed labdane diterpenoid, (4R,5S,9S,10R)‐13‐des‐ethyl‐13‐oxolabda‐8(17),11E‐dien‐19‐oic acid (1), together with nine known diterpenoids (2–3, 6–12), two lignans (4, 5),and a coumarin (13). The structures of all the compounds were elucidated on the basis ofspectrometric data, primarily one‐dimensional (1D)‐ and two‐dimensional (2D)‐NMR and massspectrometry. Electronic circular dichroism (ECD) calculations determined the absoluteconfiguration of 1. In addition, the isolated compounds were evaluated for their cytotoxic activityagainst three human tumor cell lines (HepG2, MCF‐7, and HeLa). 6,12‐Dihydroxyabieta‐5,8,11,13‐tetraen‐7‐one (6) showed moderate cytotoxicity against all three cell lines with IC50 values rangingfrom 24.41 μM to 58.39 μM and trilobinone (10) showed weaker activity with IC50 values rangingfrom 56.93 μM to 79.98 μM. None of the isolated diterpenoids have been previously reported fromJuniperus oblonga, and five compounds are here reported from the genus Juniperus for the first time.

Characterization of MGI 114 (HMAF) histiospecific toxicity in human tumor cell lines

1999 ◽  
Vol 44 (3) ◽  
pp. 235-240 ◽  
Author(s):  
Michael J. Kelner ◽  
Trevor C. McMorris ◽  
Mark A. Montoya ◽  
Leita Estes ◽  
Sheldon F. Uglik ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Human Tumor ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines ◽  
Mgi 114

scholarly journals Synthesis and Characterization of New Palladium(II) Thiosemicarbazone Complexes and Their Cytotoxic Activity against Various Human Tumor Cell Lines

2013 ◽  
Vol 2013 ◽  
pp. 1-12 ◽  
Author(s):  
Wilfredo Hernández ◽  
Juan Paz ◽  
Fernando Carrasco ◽  
Abraham Vaisberg ◽  
Evgenia Spodine ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Human Tumor ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines ◽  
Thiosemicarbazone Complexes ◽  
Benzaldehyde Thiosemicarbazone

The palladium(II) bis-chelate complexes of the type [Pd(TSC1-5)2] (6–10), with their corresponding ligands 4-phenyl-1-(acetone)-thiosemicarbazone, HTSC1(1), 4-phenyl-1-(2′-chloro-benzaldehyde)-thiosemicarbazone, HTSC2(2), 4-phenyl-1-(3′-hydroxy-benzaldehyde)-thiosemicarbazone, HTSC3(3), 4-phenyl-1-(2′-naphthaldehyde)-thiosemicarbazone, HTSC4(4), and 4-phenyl-1-(1′-nitro-2′-naphthaldehyde)-thiosemicarbazone, HTSC5(5), were synthesized and characterized by elemental analysis and spectroscopic techniques (IR and1H- and13C-NMR). The molecular structure of HTSC3, HTSC4, and [Pd(TSC1)2] (6) have been determined by single crystal X-ray crystallography. Complex6shows a square planar geometry with two deprotonated ligands coordinated toPdIIthrough the azomethine nitrogen and thione sulfur atoms in acisarrangement. Thein vitrocytotoxic activity measurements indicate that the palladium(II) complexes (IC50=0.01–9.87 μM) exhibited higher antiproliferative activity than their free ligands (IC50=23.48–70.86 and >250 μM) against different types of human tumor cell lines. Among all the studied palladium(II) complexes, the [Pd(TSC3)2] (8) complex exhibited high antitumor activity on the DU145 prostate carcinoma and K562 chronic myelogenous leukemia cells, with low values of the inhibitory concentration (0.01 and 0.02 μM, resp.).Corrigendum to “Synthesis and Characterization of New Palladium(II) Thiosemicarbazone Complexes and Their Cytotoxic Activity against Various Human Tumor Cell Lines”

Anticancer activity in murine and human tumor cell lines of bis(platinum) complexes incorporating straight-chain aliphatic diamine linker groups

1992 ◽  
Vol 35 (24) ◽  
pp. 4526-4532 ◽  
Author(s):  
Alan J. Kraker ◽  
James D. Hoeschele ◽  
William L. Elliott ◽  
H. D. Hollis Showalter ◽  
Anthony D. Sercel ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Human Tumor ◽  
Platinum Complexes ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Straight Chain ◽  
Human Tumor Cell Lines ◽  
Aliphatic Diamine
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