title: 1,2,4-benzothiadiazine linked pyrrolo[2,1-c][1,4]benzodiazepine conjugates: synthesis, DNA-binding affinity and cytotoxicity.
abstract: Benzothiadiazine-pyrrolobenzodiazepine conjugates linked through different alkane spacers have been prepared. These new classes of hybrid molecules exhibit cytotoxicity against many cancer cell lines. Their DNA thermal denaturation studies have been carried out and one of the compounds (4b) elevates the DNA helix melting temperature of the CT-DNA by 6.7 degrees C after incubation for 36 h.
authors.affiliation: Biotransformation Laboratory, Division of Organic Chemistry, Indian Institute of Chemical Technology, Hyderabad 500 007, India. ahmedkamal@iict.res.in
authors.forename: Ahmed
authors.initials: A
authors.lastname: Kamal
authors.forename: M Naseer A
authors.initials: MN
authors.lastname: Khan
authors.forename: K Srinivasa
authors.initials: KS
authors.lastname: Reddy
authors.forename: S Kaleem
authors.initials: SK
authors.lastname: Ahmed
authors.forename: M Shiva
authors.initials: MS
authors.lastname: Kumar
authors.forename: Aarti
authors.initials: A
authors.lastname: Juvekar
authors.forename: Subrata
authors.initials: S
authors.lastname: Sen
authors.forename: Surekha
authors.initials: S
authors.lastname: Zingde
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000378:metabolism* / Q000494:pharmacology; D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000378:metabolism* / Q000494:pharmacology; D001581:Benzothiadiazines / Q000138:chemical synthesis* / Q000378:metabolism* / Q000494:pharmacology; D001943:Breast Neoplasms / Q000188:drug therapy / Q000473:pathology; D002417:Cattle; D045744:Cell Line, Tumor; D004247:DNA / Q000378:metabolism*; D004262:DNA Restriction Enzymes / Q000737:chemistry; D004354:Drug Screening Assays, Antitumor; D005260:Female; D006801:Humans; D007202:Indicators and Reagents; D008297:Male; D009691:Nucleic Acid Denaturation / Q000187:drug effects; D011471:Prostatic Neoplasms / Q000188:drug therapy / Q000473:pathology; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D001581:Benzothiadiazines; D007202:Indicators and Reagents; D001569:Benzodiazepines; D004247:DNA; D004262:DNA Restriction Enzymes