Literature DB >> 28188067

Methylsulfonyl benzothiazoles (MSBT) derivatives: Search for new potential antimicrobial and anticancer agents.

Nitin P Lad1, Yogesh Manohar2, Malcolm Mascarenhas2, Yashwant B Pandit3, Mahesh R Kulkarni1, Rajiv Sharma2, Kavita Salkar4, Ashish Suthar4, Shivaji S Pandit5.   

Abstract

A series of novel 4 and 5-substituted methylsulfonyl benzothiazole (MSBT) compounds having amide, alkoxy, sulfonamide, nitro and amine functionality were synthesized from sequential reactions on 5-ethoxy-2-(methylsulfonyl)benzo[d]thiazole such as nitration, reduction, sulfonation, dealkylation, etc. All synthesized compounds were screened against antimicrobial and selected screened for anticancer activity. Antimicrobial activities studies reveled that among all compounds screened, out of MSBT-07, MSBT-11, MSBT-12, MSBT-14, MSBT-19, and MSBT-27 were found to have promising antimicrobial activity at MIC range of 4-50μg/ml against selected bacterial as well as fungal species. Compounds having good antimicrobial activity were screened for cervical cancer (HeLA cell lines). Of these MSBT-07 and MSBT-12 significantly reduced the cell growth. Consequently their calculated GI50 values were found to be 0.1 or <0.1μM.
Copyright © 2016 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Anticancer; Antimicrobial; Methylsulfonyl benzothiazoles; Nitration; Sulfonation

Mesh:

Substances:

Year:  2016        PMID: 28188067     DOI: 10.1016/j.bmcl.2016.08.032

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  5 in total

1.  Screening and Molecular Docking of Novel Benzothiazole Derivatives as Potential Antimicrobial Agents.

Authors:  Mohamed A Morsy; Enas M Ali; Mahmoud Kandeel; Katharigatta N Venugopala; Anroop B Nair; Khaled Greish; Mahmoud El-Daly
Journal:  Antibiotics (Basel)       Date:  2020-04-29

2.  Synthesis of Novel Benzazole Derivatives and Evaluation of Their Antidepressant-Like Activities with Possible Underlying Mechanisms.

Authors:  Gamze Tokgöz; Ümide Demir Özkay; Derya Osmaniye; Nazlı Turan Yücel; Özgür Devrim Can; Zafer Asım Kaplancıklı
Journal:  Molecules       Date:  2018-11-05       Impact factor: 4.411

Review 3.  Pharmaceutical and medicinal significance of sulfur (SVI)-Containing motifs for drug discovery: A critical review.

Authors:  Chuang Zhao; K P Rakesh; L Ravidar; Wan-Yin Fang; Hua-Li Qin
Journal:  Eur J Med Chem       Date:  2018-11-22       Impact factor: 6.514

4.  Synthesis and Antidepressant Activity Profile of Some Novel Benzothiazole Derivatives.

Authors:  Ümide Demir Özkay; Ceren Kaya; Ulviye Acar Çevik; Özgür Devrim Can
Journal:  Molecules       Date:  2017-09-07       Impact factor: 4.411

Review 5.  Benzothiazole derivatives as anticancer agents.

Authors:  Ali Irfan; Fozia Batool; Syeda Andleeb Zahra Naqvi; Amjad Islam; Sameh M Osman; Alessio Nocentini; Siham A Alissa; Claudiu T Supuran
Journal:  J Enzyme Inhib Med Chem       Date:  2020-12       Impact factor: 5.051

  5 in total

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