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

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.

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

Journal of Chemical Research ◽

10.1177/17475198211051910 ◽

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.

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Synthesis and Biological Evaluation of Amidinourea and Triazine Congeners as Inhibitors of MDA-MB-231 Human Breast Cancer Cell Proliferation

ChemMedChem ◽

10.1002/cmdc.201600580 ◽

2017 ◽

Vol 12 (4) ◽

pp. 288-291 ◽

Cited By ~ 2

Author(s):

Rosemary Bass ◽

Sarah Jenkinson ◽

Jennifer Wright ◽

Tora Smulders-Srinivasan ◽

Jamie C. Marshall ◽

...

Keyword(s):

Breast Cancer ◽

Cell Proliferation ◽

Breast Cancer Cell ◽

Human Breast Cancer ◽

Biological Evaluation ◽

Human Breast Cancer Cell ◽

Cancer Cell Proliferation ◽

Human Breast ◽

Breast Cancer Cell Proliferation ◽

Synthesis And Biological Evaluation

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

RSC Advances ◽

10.1039/c5ra00177c ◽

2015 ◽

Vol 5 (37) ◽

pp. 29456-29466 ◽

Cited By ~ 7

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.

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