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Molecules
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Recent Advances in the Synthesis and Biological Studies of Azaheterocycles
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Recent Advances in the Synthesis and Biological Studies of Azaheterocycles

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Organic Chemistry".

Deadline for manuscript submissions: closed (30 November 2023) | Viewed by 2355

Special Issue Editor

Dr. Mohammad Alam

E-Mail Website
Guest Editor
Department of Chemistry and Physics, Arkansas State University, Jonesboro, AR, USA
Interests: antimicrobials; anticancer agents; thiazole; pyrazole; heterocycles
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Azaheterocycles (e.g., pyrrole, imidazole, pyrazole, triazole, pyridine, pyrimidine, thiazole, etc.) comprise the core structure of a number drug molecules, and they are frequently occurring motifs in many biologically active compounds and natural products. Moreover, these heterocycles have found numerous applications in agrochemicals, dyes, fluorescent materials, and more. Hence, there is ongoing interest in azaheterocyclic chemistry recently, which is reflected by a plethora of correspondent publications.

In this respect, researchers in the field are cordially invited to submit their manuscripts relevant to the synthesis of azaheterocycles, their functionalization and their use in the construction of condensed systems for a Special Issue, ‘Recent Advances in the Synthesis and Biological Studies of Azaheterocycle Derivatives’, within the journal Molecules. Compounds with antimicrobial and anticancer properties are especially welcome in this Special Issue.

Dr. Mohammad Alam
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • pyrazole
  • thiazole
  • pyridine
  • pyrimidine
  • synthesis
  • antimicrobacterial
  • anticancer
  • anti-inflammatory

Published Papers (1 paper)

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Research

17 pages, 2819 KiB  
Article
Modulation Effect on Tubulin Polymerization, Cytotoxicity and Antioxidant Activity of 1H-Benzimidazole-2-Yl Hydrazones
by Maria Argirova, Maya Guncheva, Georgi Momekov, Emiliya Cherneva, Rositsa Mihaylova, Miroslav Rangelov, Nadezhda Todorova, Petko Denev, Kameliya Anichina, Anelia Mavrova and Denitsa Yancheva
Molecules 2023, 28(1), 291; https://doi.org/10.3390/molecules28010291 - 29 Dec 2022
Cited by 4 | Viewed by 1906
Abstract
1H-benzimidazol-2-yl hydrazones with varying hydroxy and methoxy phenyl moieties were designed. Their effect on tubulin polymerization was evaluated in vitro on porcine tubulin. The compounds elongated the nucleation phase and slowed down the tubulin polymerization comparably to nocodazole. The possible binding modes of [...] Read more.
1H-benzimidazol-2-yl hydrazones with varying hydroxy and methoxy phenyl moieties were designed. Their effect on tubulin polymerization was evaluated in vitro on porcine tubulin. The compounds elongated the nucleation phase and slowed down the tubulin polymerization comparably to nocodazole. The possible binding modes of the hydrazones with tubulin were explored by molecular docking at the colchicine binding site. The anticancer activity was evaluated against human malignant cell lines MCF-7 and AR-230, as well as against normal fibroblast cells 3T3 and CCL-1. The compounds demonstrated a marked antineoplastic activity in low micromolar concentrations in both screened in vitro tumor models. The most active were the trimethoxy substituted derivative 1i and the positional isomers 1j and 1k, containing hydroxy and methoxy substituents: they showed IC50 similar to the reference podophyllotoxin in both tumor cell lines, accompanied with high selectivity towards the malignantly transformed cells. The compounds exerted moderate to high ability to scavenge peroxyl radicals and certain derivatives—1l containing metha-hydroxy and para-methoxy group, and 1b-e with di/trihydroxy phenyl moiety, revealed HORAC values high or comparable to those of well-known phenolic antioxidants. Thus the 1H-benisimidazol-2-yl hydrazones with hydroxy/methoxy phenyl fragments were recognized as new agents exhibiting promising combined antioxidant and antineoplastic action. Full article
(This article belongs to the Special Issue Recent Advances in the Synthesis and Biological Studies of Azaheterocycles)
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