Abstract
Our current goal is the synthesis of polyheterocyclic compounds starting from 3-amino-[1,2,4]triazino[5,6-b]indole 1 and studying their anticancer activity to determine whether increasing of the size of the molecules increases the anticancer activity or not. 1-Amino[1,2,4]triazino[3′,4′:3,4]-[1,2,4]triazino[5,6-b]indole-2-carbonitrile (4) was prepared by the diazotization of 3-amino[1,2,4]-triazino[5,6-b]indole 1 followed by coupling with malononitrile in basic medium then cyclization under reflux to get 4. Also, new fused pyrimido[4″,5″:5′,6′][1,2,4]triazino-[3′,4′:3,4][1,2,4]triazino[5,6-b]indole derivative 6 was prepared and used to obtain polycyclic heterocyclic systems. Confirmation of the synthesized compounds’ structures was carried out using elemental analyses and spectral data (IR, 1H-NMR and 13C-NMR and mass spectra). The anticancer activity of some of the synthesized compounds was tested against HepG2, HCT-116 and MCF-7 cell lines. The anticancer screening results showed that some derivatives display good activity which was more potent than that of the reference drug used. Molecular docking was used to predict the binding between some of the synthesized compounds and the prostate cancer 2q7k hormone and breast cancer 3hb5 receptors.
Highlights
IntroductionWe are seeing the emergence of a new generation of drugs with hybrid molecular architectures combining the biological features of two or more small molecules
We are seeing the emergence of a new generation of drugs with hybrid molecular architectures combining the biological features of two or more small molecules.The expectation is that, in the long term, such molecular conjugates could become a dominant form of targeted infectious diseases
We succeeded in constructing many small 1,2,4-triazine molecules that had a remarkable biological activity on cancer cells [1,2]
Summary
We are seeing the emergence of a new generation of drugs with hybrid molecular architectures combining the biological features of two or more small molecules. One of the present goals in heterocyclic compound synthesis is the construction of macromolecules, in particular, by using of sequential reactions [11]. Such molecular explorations, yielding novel architectures, are of particular interest for the investigation of new bioactive agents with possible new modes of action, which could subsequently be elaborated in medicinal chemistry programs [12]. Molecules 2018, 23, x these synthetic goals have often been explored in the context of complex multistep syntheses of of natural product targets [13].
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