Synthesis of (Z)-(arylamino)-pyrazolyl/isoxazolyl-2-propenones as tubulin targeting anticancer agents and apoptotic inducers

2015 ◽  
Vol 13 (11) ◽  
pp. 3416-3431 ◽  
Author(s):  
Ahmed Kamal ◽  
Vangala Santhosh Reddy ◽  
Anver Basha Shaik ◽  
G. Bharath Kumar ◽  
M. V. P. S. Vishnuvardhan ◽  
...  
Keyword(s):  
Cell Growth ◽  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Antiproliferative Activity ◽  
Human Cancer ◽  
Tubulin Polymerization ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
New Class

A new class of pyrazole conjugates were synthesized and evaluated for their antiproliferative activity in human cancer cell lines: 9a, 9b and 9f significantly inhibited cell growth as well as tubulin polymerization.

Pyrazole–oxadiazole conjugates: synthesis, antiproliferative activity and inhibition of tubulin polymerization

2014 ◽  
Vol 12 (40) ◽  
pp. 7993-8007 ◽  
Author(s):  
Ahmed Kamal ◽  
Anver Basha Shaik ◽  
Sowjanya Polepalli ◽  
Vangala Santosh Reddy ◽  
G. Bharath Kumar ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Antiproliferative Activity ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Tubulin Polymerization ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines

A library of pyrazole–oxadiazole conjugates were synthesized and investigated for their antiproliferative activity in human cancer cell lines.

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.

Synthesis, Antiproliferative activity, and apoptotic profile of New Derivatives from the Meta Stable Benzoxazinone Scaffold

2021 ◽  
Vol 21 ◽  
Author(s):  
Amira El-Sayed ◽  
Maher El-Hashash ◽  
Wael El-Sayed
Keyword(s):  
Cell Cycle ◽  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Antiproliferative Activity ◽  
Human Cancer ◽  
Human Fibroblasts ◽  
Cancer Cell Lines ◽  
Selectivity Index ◽  
Human Cancer Cell Lines

Background: Cancer exerts a huge strain on the health system. The emerging resistance to the current chemotherapies demands the continuous development of new anticancer agents with lower cost, higher efficacy, and greater specificity. Objective: Development of selective small molecules targeted anticancer agents Methods: The behavior of benzoxazinone 2 towards nitrogen nucleophiles such as hydrazine hydrate, formamide, ethanolamine, aromatic amines, and thiosemcarbazide was described. The behavior of the amino quinazolinone 3 towards carbon electrophiles and P2S5 was also investigated. The antiproliferative activity of 17 new benzoxazinone derivatives was examined against the growth of three human cancer cell lines; liver HepG2, breast MCF-7, and colon HCT-29, in addition to the normal human fibroblasts WI-38 and the selectivity index was calculated. The possible molecular pathways such as the cell cycle and apoptosis were investigated. Results: Derivatives 3, 7, 8, 10, 13, and 15 had a significant (less than 10 µM) antiproliferative activity against the three cancer cell lines investigated. Derivative 7 showed the best antiproliferative profile comparable to that of doxorubicin. The selectivity index for all the effective derivatives ranged from ~5-12 folds indicating high selectivity against the cancer cells. Derivative 15 caused ~ 7-fold and 8-fold inductions in the expression of p53 and caspase3, respectively. It also caused a ~ 60% reduction in the expression of both topoisomerase II (topoII) and cyclin-dependent kinase 1 (cdk1). Derivatives 3, 7, and 8 had a similar profile; ~ 6-8-fold increases in the expression of p53 and caspase3 but these compounds were devoid of any significant effect on the expression of topoII and cdk1. Derivatives 10 and 13 were also similar and resulted in a ~6-fold elevation in the expression of caspase3, and more than 60% downregulation in the expression of topoII. The results of the gene expression of topoII and caspase 3 were confirmed by the measurement of the topoII concentration and caspase3 activity in the HepG2 cells. Conclusion: Six derivatives exerted their antiproliferative activity by arresting the cell cycle (decreasing cdk1), preventing the DNA duplication (downregulating topo II), and by inducing apoptosis (inducing p53 and caspase3). One common feature in all the six active derivatives is the presence of free amino group. These compounds have merit for further investigations.

scholarly journals Synthetic Sphingolipids with 1,2-Pyridazine Appendages Improve Antiproliferative Activity in Human Cancer Cell Lines

2020 ◽  
Vol 11 (5) ◽  
pp. 686-690 ◽  
Author(s):  
Sylvestre P. J. T. Bachollet ◽  
Vito Vece ◽  
Alison N. McCracken ◽  
Brendan T. Finicle ◽  
Elizabeth Selwan ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Antiproliferative Activity ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines

scholarly journals Antiproliferative Oleanane Saponins from Polyscias Guilfoylei

2008 ◽  
Vol 3 (10) ◽  
pp. 1934578X0800301 ◽  
Author(s):  
Giuseppina Cioffi ◽  
Antonio Vassallo ◽  
Laura Lepore ◽  
Fabio Venturella ◽  
Fabrizio Dal Piaz ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Antiproliferative Activity ◽  
Human Cancer ◽  
2D Nmr ◽  
Human Cancer Cell ◽  
Hek 293 ◽  
Human Cancer Cell Lines ◽  
Echinocystic Acid ◽  
Aerial Parts

Three new oleanane saponins (1–3), together with four known ones (4–7), were isolated from the aerial parts of Polyscias guilfoylei. Their structures were elucidated by 1D and 2D NMR experiments, including 1D TOCSY, DQF-COSY, ROESY, HSQC, and HMBC spectroscopy, as well as ESIMS analysis. The antiproliferative activity of all compounds was evaluated using three murine and human cancer cell lines; J774.A1, HEK-293, and WEHI-164. All the compounds were inactive except for 3β- O-[β-D-glucopyranosyl-(1→2)-α-L-arabinopyranosyl]-echinocystic acid 28-[ O-β-D-glucopyranosyl-(1→6) O-β-D-glucopyranosyl] ester (3), which was active against all the cell lines.

scholarly journals Design and synthesis of substituted (1-(benzyl)-1H-1,2,3-triazol-4-yl)(piperazin-1-yl)methanone conjugates: study on their apoptosis inducing ability and tubulin polymerization inhibition

2020 ◽  
Vol 11 (11) ◽  
pp. 1295-1302
Author(s):  
Kesari Lakshmi Manasa ◽  
Sowjanya Thatikonda ◽  
Dilep Kumar Sigalapalli ◽  
Sowmya Vuppaladadium ◽  
Ganthala Parimala Devi ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Proliferative Potential ◽  
Tubulin Polymerization ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Design And Synthesis ◽  
Substituted 1

Herein, we have designed and synthesized a library of substituted (1-(benzyl)-1H-1,2,3-triazol-4-yl)(piperazin-1-yl)methanone derivatives (10aa–ef) and evaluated for their anti-proliferative potential against a panel of human cancer cell lines.

Antiproliferative activity of Hungarian Asteraceae species against human cancer cell lines. Part II

2009 ◽  
Vol 23 (8) ◽  
pp. 1109-1115 ◽  
Author(s):  
Boglárka Csupor-Löffler ◽  
Zsuzsanna Hajdú ◽  
Borbála Réthy ◽  
István Zupkó ◽  
Imre Máthé ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Antiproliferative Activity ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines
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