One-pot synthesis and biological evaluation of (2E,4E)-4-arylidene-2-styryl-5-oxopyrrolidine derivatives

2021 ◽  
pp. 174751982110519
Author(s):  
Ling-Qi Kong ◽  
Xiu-Lian Zhu ◽  
Qin-Hua Chen ◽  
Lun Wu ◽  
Hong-Mei Wang ◽  
...  
Keyword(s):  
Cell Proliferation ◽  
Hepg2 Cells ◽  
Biological Evaluation ◽  
Cancer Cell Proliferation ◽  
Marine Alkaloids ◽  
Antitumor Activities ◽  
One Pot ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of ◽  
Mtt Assays

Many marine alkaloids possess interesting structures and antitumor activities. Thus, we have synthesized (2 E,4 E)-4-arylidene-2-styryl-5-oxopyrrolidine derivatives of the marine alkaloids, rhopaladins A–D. The cytotoxicities of these derivatives against C-33A, CaSki, SiHa, HeLa, HepG2, and LO2 cells are evaluated by MTT assays. The results show that (2 E,4 E)-2-(4-chlorostyryl)-4-benzylidene- N-cyclohexyl-1-(4-fluorophenyl)-5-oxopyrrolidine-2-carboxamide significantly inhibits cancer cell proliferation, with IC50 values against C-33A, CaSki, SiHa, HeLa, and HepG2 cells of 5.56, 9.15, 12.5, 21.4, and 14.5 μM, respectively, and an IC50 value of 86.77 μM against the normal LO2 cell line.

scholarly journals Synthesis and Biological Evaluation of New Glycoconjugated LDH Inhibitors as Anticancer Agents

Molecules ◽  
2019 ◽  
Vol 24 (19) ◽  
pp. 3520 ◽  
Author(s):  
Felicia D’Andrea ◽  
Giulia Vagelli ◽  
Carlotta Granchi ◽  
Lorenzo Guazzelli ◽  
Tiziano Tuccinardi ◽  
...  
Keyword(s):  
Cell Proliferation ◽  
Anticancer Agents ◽  
Biological Response ◽  
Biological Evaluation ◽  
Biologically Active ◽  
Cancer Cell Proliferation ◽  
Structural Variations ◽  
Lactate Formation ◽  
Synthesis And Biological Evaluation ◽  
Sugar Stereochemistry

Conjugation of known biologically active molecules to carbohydrate frameworks represents a valuable option for the preparation of hybrid, structurally-related families of compounds with the aim of modulating their biological response. Therefore, we present here a study on the preparation of d-galacto, d-manno, d-gluco, and d-lactose glycoconjugates of an established N-hydroxyindole-based (NHI) inhibitor of lactated dehydrogenase (LDH). Structural variations involved the sugar stereochemistry and size as well as the anchoring point of the NHI on the carbohydrate frame (either C-1 or C-6). In the case of the galactose anomeric glycoconjugate (C-1), intriguing solvent-dependent effects were observed in the glycosylation stereochemical outcome. The biological activity of the deprotected glycoconjugates in contrasting lactate formation and cancer cell proliferation are described.

Design, synthesis and biological evaluation of novel C3-functionalized oxindoles as potential Pim-1 kinase inhibitors

RSC Advances ◽  
2015 ◽  
Vol 5 (37) ◽  
pp. 29456-29466 ◽  
Author(s):  
Hong-bao Sun ◽  
Xiao-yan Wang ◽  
Guo-bo Li ◽  
Li-dan Zhang ◽  
Jie Liu ◽  
...  
Keyword(s):  
Cell Proliferation ◽  
Cancer Cell ◽  
Kinase Inhibitors ◽  
Human Cancer ◽  
Biological Evaluation ◽  
Cancer Cell Proliferation ◽  
Human Cancer Cell ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

A novel series of C3-functionalized oxindoles, 3-(2-oxo-4-phenylbut-3-en-1-ylidene) indolin-2-ones as potential Pim-1 kinase inhibitors, were designed, synthesized and investigated for inhibition of human cancer-cell proliferation.

Design, Synthesis and Biological Evaluation of Novel Aminosaccharide Derivatives of Combretastatin A-4

2013 ◽  
Vol 10 (10) ◽  
pp. 935-941
Author(s):  
Yan Tang ◽  
Zhewei Tu ◽  
Jing Sun ◽  
Xiong Zhu ◽  
Kun Liu ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

scholarly journals Molecular modeling study, synthesis and biological evaluation of combretastatin A-4 analogues as anticancer agents and tubulin inhibitors

MedChemComm ◽  
2018 ◽  
Vol 9 (2) ◽  
pp. 316-327 ◽  
Author(s):  
Yang Ping Quan ◽  
Li Ping Cheng ◽  
Tian Chi Wang ◽  
Wan Pang ◽  
Fan Hong Wu ◽  
...  
Keyword(s):  
Molecular Modeling ◽  
Anticancer Agents ◽  
Hepg2 Cells ◽  
Binding Mode ◽  
Biological Evaluation ◽  
Tubulin Inhibitors ◽  
Molecular Modeling Study ◽  
Synthesis And Biological Evaluation ◽  
Modeling Study

Compound 13a, more effective than CA-4 against HepG2 cells and tubulin, and the proposed binding mode for 13a.

Synthesis, characterization and in vitro and in vivo anticancer activity of Pt(iv) derivatives of [Pt(1S,2S-DACH)(5,6-dimethyl-1,10-phenanthroline)]

2017 ◽  
Vol 46 (21) ◽  
pp. 7005-7019 ◽  
Author(s):  
Benjamin W. J. Harper ◽  
Emanuele Petruzzella ◽  
Roman Sirota ◽  
Fernanda Fabiola Faccioli ◽  
Janice R. Aldrich-Wright ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

Synthesis and biological evaluation in vitro and in vivo of functionalized Pt(iv) derivatives of Pt56MeSS.

Design, Synthesis, and Biological Evaluation of Novel Fluoro Derivatives of BCNA

2009 ◽  
Vol 82 (2) ◽  
pp. A57
Author(s):  
Marco Derudas ◽  
Maurizio Quintiliani ◽  
Christopher McGuigan ◽  
Andrea Brancale ◽  
Geoffrey Henson ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of ◽  
Fluoro Derivatives

scholarly journals Synthesis and biological evaluation of 4-substituted aryl-piperazine derivatives of 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo [5.2.1.02,6] dec-8-ene-3,5-dione as anti-cancer and anti-angiogenesis agents

2020 ◽  
Author(s):  
Lifang Guo ◽  
Benshan Xu ◽  
Zirui Wan ◽  
Lulu Ren ◽  
Jie Zhang ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Cytotoxic Activities ◽  
Chemical Structures ◽  
Piperazine Derivatives ◽  
Anti Cancer ◽  
Ic50 Values ◽  
And Migration ◽  
Anti Tumor Activity ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

Abstract Background: A series of aryl-piperazine derivatives of 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo [5.2.1.02,6] dec-8-ene-3,5-dione were synthesized. The chemical structures of the desired compounds were identified by 1H NMR, ESI-MS and elementary analytical. The anti-cancer and anti-angiogenesis activities of the newly synthesized compounds were evaluated by proliferation and migration assays, respectively. Results: The screening results demonstrated that compounds 2 and 5 showed potent anti-tumor activity (IC50 values ranging from 7.1 to 15.9μM) with low cytotoxic activities (IC50＞79.3μM). Although compound 5 showed little effects on endothelia proliferation (IC50=65.3μM), it indeed significantly abrogated endothelia cell migration (IC50=6.7μM). Conclusions: This work may impart new direction for the investigations of aryl-piperazine derivatives and lead to the development of potent novel anti-tumor and anti-angiogenesis agents.

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