Related Experiment Video
Updated: Aug 9, 2026

Synthesis and Bioconjugation of Thiol-Reactive Reagents for the Creation of Site-Selectively Modified Immunoconjugates
Published on: March 6, 2019
Synthesis of aminoacyl thiaolidones as potential antitumour agents
Ana Cristina Lima Leite1, Luciene Maria F Santos, Fábio Fernandes Barbosa
1Laboratório de Planejamento, Avaliação e Síntese de Fármacos, LABSINFA, Departamento de Ciências Farmacêuticas, Universidade Federal de Pernambuco, Rua Prof. Artur Sa, S/N, CDU, Recife, Pernambuco, Brazil. acllb@yahoo.com.br
Abstract:
In the scope of a research program aiming to perform the synthesis and pharmacological evaluation of novel possible antitumour prototype compounds, we report in this paper the synthesis of new peptidyl derivatives from 4-thiazolidone nucleus. The synthesis reactions have been performed based in peptide synthesis as strategies. The characterisation of this new class of compounds was performed with IR and (1)H-NMR spectroscopy. In vivo, antitumour activity tests showed that some of these compounds were able to inhibit significantly sarcoma S-180 tumour growth in mice, revealing itself as a new potential class of drugs in cancer chemotherapy.
Related Concept Videos
Preparation of 1° Amines: Azide Synthesis
Azide ions act as good nucleophiles and react with unhindered alkyl halides to form alkyl azides. Alkyl azides do not participate in further nucleophilic substitution reactions, thereby eliminating the chances of polyalkylated products. Alkyl azides are reduced by hydride-based reducing agents, like lithium aluminum...
Preparation of 1° Amines: Gabriel Synthesis
Strong bases like NaOH or KOH deprotonate the phthalimide to form the corresponding anion, which acts as a nucleophile. Further, the anion attacks an...
Aryldiazonium Salts to Azo Dyes: Diazo Coupling
Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase
Preparation of Amides
The DCC-promoted synthesis of amides begins with the protonation of DCC by carboxylic acid. The protonation makes it a better acceptor. Next, the addition of carboxylate to the protonated carbodiimide gives a reactive acylating agent.
Subsequently, the amine acts as a nucleophile that attacks the acylating agent to form a tetrahedral intermediate. In the...
Amino Acid Biosynthetic Pathways