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

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

  • Bioorg Med Chem Lett. 2017 Mar 1;27(5):1319-1324. doi: 10.1016/j.bmcl.2016.08.032.
Nitin P Lad 1,  Yogesh Manohar 2,  Malcolm Mascarenhas 2,  Yashwant B Pandit 3,  Mahesh R Kulkarni 1,  Rajiv Sharma 2,  Kavita Salkar 4,  Ashish Suthar 4,  Shivaji S Pandit 5
Affiliations

Affiliations

  • 1 Research Centre and Post Graduate Department of Chemistry, Padmashri Vikhe Patil College of Arts, Science and Commerce, Pravaranagar, A/P Loni, Tal. Rahata, Dist. Ahmednagar 413713, India; Department of Medicinal Chemistry, Piramal Enterprises Ltd, 1-Nirlon Complex, Goregaon (East), Mumbai 400063, India.
  • 2 Department of Medicinal Chemistry, Piramal Enterprises Ltd, 1-Nirlon Complex, Goregaon (East), Mumbai 400063, India.
  • 3 Applied Chemistry Division, DIAT-DRDO, Girinagar, Pune 411025, India.
  • 4 Department of Phytomedicines, Piramal Enterprises Ltd, 1-Nirlon Complex, Goregaon (East), Mumbai 400063, India.
  • 5 Research Centre and Post Graduate Department of Chemistry, Padmashri Vikhe Patil College of Arts, Science and Commerce, Pravaranagar, A/P Loni, Tal. Rahata, Dist. Ahmednagar 413713, India.
PMID: 28188067 DOI: 10.1016/j.bmcl.2016.08.032
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.

Keywords

Anticancer; Antimicrobial; Methylsulfonyl benzothiazoles; Nitration; Sulfonation.

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