Synthesis of C8-linked pyrrolo[2,1-c][1,4]benzodiazepine-benzimidazole conjugates with remarkable DNA-binding affinity.
Two types of benzimidazoles have been synthesized and linked to DC-81 at C8-position through different alkyl chain spacers. These PBD conjugates have exhibited remarkable DNA-binding affinity, and a representative compound shows promising in vitro anticancer activity.
Kamal
Ahmed
A
Division of Organic Chemistry, Indian Institute of Chemical Technology, Hyderabad 500007, India. ahmedkamal@iict.res.in
Ramulu
P
P
Srinivas
O
O
Ramesh
G
G
Kumar
P Praveen
PP
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001562:Benzimidazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001569:Benzodiazepines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004247:DNA / Q000737:chemistry / Q000187:drug effects / Q000378:metabolism*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009691:Nucleic Acid Denaturation; D011758:Pyrroles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013950:Thymus Gland / Q000378:metabolism
D000970:Antineoplastic Agents; D001562:Benzimidazoles; D011758:Pyrroles; C438462:pyrrolo(2,1-c)(1,4)benzodiazepine; D001569:Benzodiazepines; D004247:DNA