title: Solid-phase synthesis of new pyrrolobenzodiazepine-chalcone conjugates: DNA-binding affinity and anticancer activity.
abstract: A new class of C8-linked pyrrolo[2,1-c][1,4]benzodiazepine-chalcone conjugates have been prepared by employing a solid-phase synthetic protocol. In this strategy an intramolecular aza-Wittig reductive cyclization approach has been utilized. Interestingly, some of these molecules have shown enhanced DNA-binding affinity and promising anticancer activity on a large number of human cancer cell lines.
authors.affiliation: Chemical Biology Laboratory, Division of Organic Chemistry, Indian Institute of Chemical Technology, Hyderabad, Andra Pradesh 500 007, India. ahmedkamal@iict.res.in
authors.forename: Ahmed
authors.initials: A
authors.lastname: Kamal
authors.forename: N
authors.initials: N
authors.lastname: Shankaraiah
authors.forename: S
authors.initials: S
authors.lastname: Prabhakar
authors.forename: Ch Ratna
authors.initials: ChR
authors.lastname: Reddy
authors.forename: N
authors.initials: N
authors.lastname: Markandeya
authors.forename: K Laxma
authors.initials: KL
authors.lastname: Reddy
authors.forename: V
authors.initials: V
authors.lastname: Devaiah
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D001569:Benzodiazepines / Q000138:chemical synthesis / Q000494:pharmacology*; D001665:Binding Sites; D045744:Cell Line, Tumor / Q000187:drug effects*; D002599:Chalcone / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology*; D004247:DNA / Q000737:chemistry / Q000378:metabolism*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008956:Models, Chemical; D011758:Pyrroles / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D011758:Pyrroles; C438462:pyrrolo(2,1-c)(1,4)benzodiazepine; D001569:Benzodiazepines; D002599:Chalcone; D004247:DNA