Discovery and investigation of 1-[4-(2-aminoethoxy)phenylcarbonyl]-3,5-bis-(benzylidene)-4-piperidones as candidate antineoplastic agents: Our last 15 years study.

doi:10.2174/0929867327666200730215752

Paper

Discovery and investigation of 1-[4-(2-aminoethoxy)phenylcarbonyl]-3,5-bis-(benzylidene)-4-piperidones as candidate antineoplastic agents: Our last 15 years study.

Published Jul 30, 2020 · Mohammad Hossain, Carlos E Enci, J. Dimmock

Current medicinal chemistry

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5

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Abstract

This review outlines the discovery and development of a novel series of 1-[4-2-aminoethoxy)phenylcarbonyl]- 3,5-bis-(benzylidene)-4-piperidones 5-8 as potential drug candidates over the last 15 years in our laboratory. Many of these compounds demonstrate excellent cytotoxic properties and are often more potent than contemporary anticancer drugs. Two highly important features of many of these molecules are first, the greater tumour-selective toxicity and second, the ability of these molecules to act as modulators of multi-drug resistance. The modes of action of some of the potent compounds are by apoptosis induction, generation of reactive oxygen species, activation of certain caspases and affecting mitochondrial functions. These molecules also display promising antimalarial and antimycobacterial properties. In a short term toxicity study, these molecules are well tolerated in mice. Structure-activity relationships, and a drug delivery system along with pharmacokinetic studies and metabolic stability of these compounds have been presented. The positive characteristics associated the series 5-8 warrants their further evaluations as candidate antineoplastic drug candidates.

Literature Review

Study Snapshot

The novel series of 1-[4-(2-aminoethoxy)phenylcarbonyl]- 3,5-bis-(benzylidene)-4-piperidones 5-8 show potential as potent antineoplastic agents with tumor-selective toxicity and modulation of multi-d

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Discovery and investigation of 1-[4-(2-aminoethoxy)phenylcarbonyl]-3,5-bis-(benzylidene)-4-piperidones as candidate antineoplastic agents: Our last 15 years study.

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References

Citations

In‐Vitro Investigation of the α‐Amylase Inhibition Activity of Bare Bis‐Benzylidene‐Cyclohexanone Synthesized by a Highly Selective Solvent‐Free Route

The highly selective, solvent-free synthesis of Bis-benzylidine cyclohexanone (BBC) demonstrates 88.5 % alpha amylase inhibition activity, comparable to commercial drugs, and a new target site for drug design.

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Novel pyridine derivatives show promising anticancer properties, with compound 3b showing the highest inhibitory effect on tubulin polymerization and showing potential in vivo against breast cancer.

Cytotoxic derivatives of dichloroacetic acid and some metal complexes

DCA and its derivatives can be modified into potent cytotoxins, offering potential as promising anticancer agents.

Design, Synthesis and Tumour-Selective Toxicity of Novel 1-[3-{3,5-Bis(benzylidene)-4-oxo-1-piperidino}-3-oxopropyl]-4-piperidone Oximes and Related Quaternary Ammonium Salts

Novel 1-[3-3,5-bis(benzylidene)-4-oxo-1-piperidino-3-oxopropyl]-4-piperidone oximes and related quaternary ammonium salts show potent cytotoxicity against neoplastic cancer

Sensitivity of Acute Myelocytic Leukemia Cells to the Dienone Compound VLX1570 Is Associated with Inhibition of the Ubiquitin-Proteasome System

VLX1570 effectively inhibits the ubiquitin-proteasome system in acute myeloid leukemia cells, leading to cell death and potential therapeutic applications in cancer therapeutics.