title: Synthesis and biological evaluation of estradiol linked pyrrolo[2,1-c][1,4]benzodiazepine (PBD) conjugates as potential anticancer agents.
abstract: A series of new estradiol linked pyrrolo[2,1-c][1,4]benzodiazepine (E(2)-PBD) conjugates (3a-f, 4a-f and 5a-f) with different linker architectures including a triazole moiety have been designed and synthesized. All the 18 compounds have been evaluated for their anticancer activity and it is observed that some of the compounds particularly 4c-e and 5c,d exhibited significant anticancer activity. The detailed biological aspects relating to the cell cycle effects and tubulin depolymerization activity have been examined with a view to understand the mechanism of action of these conjugates. Among all these conjugates, one of the compound 5c could be considered as the most effective compound particularly against MCF-7 breast cancer cell line.
authors: Division of Organic Chemistry, Indian Institute of Chemical Technology, Hyderabad, India. ahmedkamal@iict.res.in
authors: Ahmed
authors: A
authors: Kamal
authors: M Kashi
authors: MK
authors: Reddy
authors: M Janaki
authors: MJ
authors: Ramaiah
authors: Rajender
authors: J Surendranadha
authors: JS
authors: Reddy
authors: Y V V
authors: YV
authors: Srikanth
authors: D
authors: D
authors: Dastagiri
authors: E Vijaya
authors: EV
authors: Bharathi
authors: S N C V L
authors: SN
authors: Pushpavalli
authors: Pranjal
authors: P
authors: Sarma
authors: Manika
authors: M
authors: Pal-Bhadra
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000494:pharmacology; D001943:Breast Neoplasms / Q000188:drug therapy / Q000473:pathology; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D004958:Estradiol; D004967:Estrogens; D005260:Female; D006801:Humans; D011758:Pyrroles; D013329:Structure-Activity Relationship; D014404:Tubulin / Q000187:drug effects
chemical_list: D000970:Antineoplastic Agents; D004967:Estrogens; D011758:Pyrroles; D014404:Tubulin; D001569:Benzodiazepines; D004958:Estradiol