Literature DB >> 21435889

Anti-tumor and anti-leishmanial evaluations of 1,3,4-oxadiazine, pyran derivatives derived from cross-coupling reactions of β-bromo-6H-1,3,4-oxadiazine derivatives.

Rafat M Mohareb1, Jürgen Schatz.   

Abstract

Cyanoacetylhydrazine reacted with the ω-bromoacetophenones 2a,b to give hydrazide-hydrazone derivatives 3a,b. The latter products were cyclized to the 1,3,4-oxadiazine derivatives 4a,b. Bromination of the latter products gave the 6-bromo-6H-1,3,4-oxadiazine derivatives 5a,b which underwent a series of cross-coupling reactions. The antitumor evaluation of the newly synthesized products against the three cancer cells namely breast adenocarcinoma (MCF-7), non-small cell lung cancer (NCI-H460) and CNS cancer (SF-268) showed that some of them have high inhibitory effect towards three cell lines which is higher than the standard. Moreover, the anti-leishmanial activity of the newly synthesized product was tested on Leishmania donovani amastigotes showed that some compounds have high activity. Crown
Copyright © 2011. Published by Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 21435889     DOI: 10.1016/j.bmc.2011.02.051

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  4 in total

1.  The cyanobacterial metabolite nocuolin a is a natural oxadiazine that triggers apoptosis in human cancer cells.

Authors:  Kateřina Voráčová; Jan Hájek; Jan Mareš; Petra Urajová; Marek Kuzma; José Cheel; Andreas Villunger; Alexandra Kapuscik; Marcel Bally; Petr Novák; Martin Kabeláč; Gerhard Krumschnabel; Martin Lukeš; Ludmila Voloshko; Jiří Kopecký; Pavel Hrouzek
Journal:  PLoS One       Date:  2017-03-02       Impact factor: 3.240

Review 2.  Developments of Cyanobacteria for Nano-Marine Drugs: Relevance of Nanoformulations in Cancer Therapies.

Authors:  Vivek K Bajpai; Shruti Shukla; Sung-Min Kang; Seung Kyu Hwang; Xinjie Song; Yun Suk Huh; Young-Kyu Han
Journal:  Mar Drugs       Date:  2018-05-23       Impact factor: 5.118

3.  Synthesis, characterization, DFT, antioxidant, antibacterial, pharmacokinetics and inhibition of SARS-CoV-2 main protease of some heterocyclic hydrazones.

Authors:  Lilia Adjissi; Nadjib Chafai; Khalissa Benbouguerra; Imene Kirouani; Abdelkader Hellal; Houdheifa Layaida; Meriem Elkolli; Chawki Bensouici; Salah Chafaa
Journal:  J Mol Struct       Date:  2022-08-23       Impact factor: 3.841

4.  Uses of cyanoacetylhydrazine in heterocyclic synthesis: novel synthesis of pyrazole derivatives with anti-tumor activities.

Authors:  Rafat M Mohareb; Nahed N E El-Sayed; Mahmoud A Abdelaziz
Journal:  Molecules       Date:  2012-07-12       Impact factor: 4.411

  4 in total

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