title: Novel hybrids of drug with bioactive heterocycles for enhancing biological activity.
abstract: A novel series of aceclofenac hybridised with 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazoles were designed using molecular hybridization approach and synthesised 6a-j. The structural integrity was confirmed by analytical methods. The hybrid molecules were subjected to in vitro cytotoxic studies against four human cancer cell lines PA-1, OAW-42, T47-D and MCF-7 by MTT assay method. The results indicate that the hybrid molecules bearing halogen on phenyl ring in 6th position of triazolo-thiadiazole exhibited significant cytotoxic activity. The test compounds were also screened for antifungal activity against two strains.
authors.affiliation: Department of Pharmaceutical Chemistry, Jaya College of Paramedical Sciences, College of Pharmacy, Thiruninravur, Chennai, Tamil Nadu, 602024, India. drpvalentina@gmail.com.
authors.forename: Parthiban
authors.initials: P
authors.lastname: Valentina
authors.affiliation: Department of Pharmaceutical Chemistry, SRM College of Pharmacy, SRM University, Kattankulathur, Kancheepuram, Tamil Nadu, 603203, India.
authors.forename: Kaliappan
authors.initials: K
authors.lastname: Ilango
authors.affiliation: Department of Pharmaceutical Chemistry, SRM College of Pharmacy, SRM University, Kattankulathur, Kancheepuram, Tamil Nadu, 603203, India.
authors.forename: Muthu K
authors.initials: MK
authors.lastname: Kathiravan
mesh_terms: D000935:Antifungal Agents / Q000737:chemistry* / Q000494:pharmacology; D001234:Aspergillus niger / Q000187:drug effects / Q000502:physiology; D001688:Biological Products / Q000737:chemistry* / Q000494:pharmacology; D002176:Candida albicans / Q000187:drug effects / Q000502:physiology; D006571:Heterocyclic Compounds / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D061986:MCF-7 Cells; D013329:Structure-Activity Relationship; D013830:Thiadiazoles / Q000737:chemistry* / Q000494:pharmacology; D014230:Triazoles / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000935:Antifungal Agents; D001688:Biological Products; D006571:Heterocyclic Compounds; D013830:Thiadiazoles; D014230:Triazoles
keywords: Cytotoxic; Molecular hybrids; Triazolo-thiadiazole