N,N-Bis(glycityl)amines as anti-cancer drugs

Waghorne, Charlotte L.; Corkran, Hilary M.; Hunt-Painter, Alex A.; Niktab, Eliatan; Baty, James W.; Berridge, Michael V.; Munkacsi, Andrew B.; McConnell, Melanie J.; Timmer, Mattie S. M.; Stocker, Bridget L.

doi:10.1016/j.bmc.2016.04.016

Cited by 6 publications

(4 citation statements)

References 18 publications

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“…Waghorne et al [5] described the design of novel chemotherapeutic agents (N,N-bis(glycityl)amines) that were prepared through the reductive amination of hexoses and pentoses and were subsequently screened for anticancer activity against cancerous virus. The amination approach was applied in the development of our novel inhibitor as shown in Fig.…”

Section: Methodsmentioning

confidence: 99%

An in silico LLPS perturbation approach in the design of a novel SARS-CoV-2 spike receptor-binding domain inhibitor

Durojaye

Sedzro

Mushiana

et al. 2020

Egypt J Med Hum Genet

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The reversible process where a homogenous fluid de-mixes into two distinctively separate liquid phases is referred to as LLPS (Liquid-liquid phase separation). The resulting liquid is made up of one dilute phase and one condensed phase. An increasing number of studies have shown that the liquid-liquid phase separation is an important principle that underlies intracellular organization in biological systems, forming liquid condensates without a membrane envelope, otherwise known as MLOs (membraneless organelles). Such organelles include the P bodies, nucleolus and stress granules. Moreover, the regulation of many other biological processes such as signal transduction, chromatin rearrangement and RNA metabolism have been linked to the liquid-liquid phase separation.

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Section: Methodsmentioning

confidence: 99%

An in silico LLPS perturbation approach in the design of a novel SARS-CoV-2 spike receptor-binding domain inhibitor

Durojaye

Sedzro

Mushiana

et al. 2020

Egypt J Med Hum Genet

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“…Cancer is the major cause of death in the present world. Approximately 14 million cancer cases was diagnosed and 8.2 million people died because of cancer in 2012 [1] [2].…”

Section: Introductionmentioning

confidence: 99%

Biological Evaluation of New Schiff Bases: Synthesized from 4-Amino-3,5-dimethyl-1,2,4-triazole, Phenathroline and Bipyridine Dicarboxaldehydes

Islam¹,

Karim²,

Boadi³

et al. 2016

ABC

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Four new Schiff bases with promising anticancer activity have been synthesized from 4-amino-3,5-dimethyl-1,2,4-triazole and di-pyridyl-aldehydes. Structures have been established by various spectroscopic methods. The compounds were tested in vitro to study their cytotoxicity and anti-oxidative activity in human lung carcinoma (A549), breast carcinoma (BT549), prostate adenocarcinoma (PC3) and mouse preadipocytes (3T3-L1) cells. Compound 1 was found to increase Glutathione (GSH) level slightly in all four cell lines. Compound 4 showed better selectivity and cytotoxicity against both BT549 and A549 cells compared to the anticancer drug tamoxifen. With the exception of compound 4 which reduced GSH levels in A549 and BT549, all other compounds maintained GSH levels in comparison to their respective controls.

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“…The International Agency for Research on Cancer reported that the global cancer burden rose to 14.1 million new cases with 8.2 million cancer deaths in 2012, and the annual incidence of new cancer cases is estimated to increase to 19.3 million by 2050 [1]. During the past few years, cyclooxygenases (COX-1 and COX-2) were introduced as novel targets for cancer treatment [2].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Biological Evaluation, Docking and QSAR Studies of Some Novel Naphthalimide Dithiocarbamate Analogs as Antitumor and Anti- Inflammatory Agents

Zahra¹,

Osman²,

Agwa³

et al. 2016

Med chem (Los Angeles)

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A series of novel naphthalimide dithiocarbamate 4a-f, 5a-f were efficiently synthesized via introduce dithiocarbamate and dithioate side chain onto the naphthalic anhydride core. The structures of the synthesized analogs were elucidated by spectroscopic methods, including IR, 1 H and 13 C NMR, and (ESIHRMS) techniques. The anti-cancer activities of the generated naphthalimide derivatives 4c, 4d, 4e, 4f, and 5d were evaluated against 21 tumour cell lines; inculding 10 tumor subpanels using MTT assay. Analogue 4c offer antitumor activity with an IC 50 of 10.54 µM against SKBR3 breast cancer cells. Compound 4d showed varying degrees of antitumor activities towards several tumour cell lines ranging from 21.1 to 71.7 µM. In addition to the antitumor activities; the synthesized compounds were evaluated for their in vitro anti-inflammatory activity. Compounds 4c and 4d revealed potent anti-inflammatory properties in comparison with the reference drug celecoxib. Molecular docking studies provided complementary theoretical support for experimental biological data.

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N,N-Bis(glycityl)amines as anti-cancer drugs

Cited by 6 publications

References 18 publications

An in silico LLPS perturbation approach in the design of a novel SARS-CoV-2 spike receptor-binding domain inhibitor

An in silico LLPS perturbation approach in the design of a novel SARS-CoV-2 spike receptor-binding domain inhibitor

Biological Evaluation of New Schiff Bases: Synthesized from 4-Amino-3,5-dimethyl-1,2,4-triazole, Phenathroline and Bipyridine Dicarboxaldehydes

Synthesis, Biological Evaluation, Docking and QSAR Studies of Some Novel Naphthalimide Dithiocarbamate Analogs as Antitumor and Anti- Inflammatory Agents

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