title: Methylsulfonyl benzothiazoles (MSBT) derivatives: Search for new potential antimicrobial and anticancer agents.
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 GI50values were found to be 0.1 or <0.1μM.
authors.affiliation: 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.
authors.forename: Nitin P
authors.initials: NP
authors.lastname: Lad
authors.affiliation: Department of Medicinal Chemistry, Piramal Enterprises Ltd, 1-Nirlon Complex, Goregaon (East), Mumbai 400063, India.
authors.forename: Yogesh
authors.initials: Y
authors.lastname: Manohar
authors.affiliation: Department of Medicinal Chemistry, Piramal Enterprises Ltd, 1-Nirlon Complex, Goregaon (East), Mumbai 400063, India.
authors.forename: Malcolm
authors.initials: M
authors.lastname: Mascarenhas
authors.affiliation: Applied Chemistry Division, DIAT-DRDO, Girinagar, Pune 411025, India.
authors.forename: Yashwant B
authors.initials: YB
authors.lastname: Pandit
authors.affiliation: 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.
authors.forename: Mahesh R
authors.initials: MR
authors.lastname: Kulkarni
authors.affiliation: Department of Medicinal Chemistry, Piramal Enterprises Ltd, 1-Nirlon Complex, Goregaon (East), Mumbai 400063, India.
authors.forename: Rajiv
authors.initials: R
authors.lastname: Sharma
authors.affiliation: Department of Phytomedicines, Piramal Enterprises Ltd, 1-Nirlon Complex, Goregaon (East), Mumbai 400063, India.
authors.forename: Kavita
authors.initials: K
authors.lastname: Salkar
authors.affiliation: Department of Phytomedicines, Piramal Enterprises Ltd, 1-Nirlon Complex, Goregaon (East), Mumbai 400063, India.
authors.forename: Ashish
authors.initials: A
authors.lastname: Suthar
authors.affiliation: 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.
authors.forename: Shivaji S
authors.initials: SS
authors.lastname: Pandit
mesh_terms: D000890:Anti-Infective Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects*; D052160:Benzothiazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D005658:Fungi / Q000187:drug effects*; D006367:HeLa Cells; D006801:Humans; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure
chemical_list: D000890:Anti-Infective Agents; D000970:Antineoplastic Agents; D052160:Benzothiazoles; C576094:methylsulfonyl benzothiazole
keywords: Anticancer; Antimicrobial; Methylsulfonyl benzothiazoles; Nitration; Sulfonation