1,2,4-benzothiadiazine linked pyrrolo[2,1-c][1,4]benzodiazepine conjugates: synthesis, DNA-binding affinity and cytotoxicity.
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.
Kamal
Ahmed
A
Biotransformation Laboratory, Division of Organic Chemistry, Indian Institute of Chemical Technology, Hyderabad 500 007, India. ahmedkamal@iict.res.in
Khan
M Naseer A
MN
Reddy
K Srinivasa
KS
Ahmed
S Kaleem
SK
Kumar
M Shiva
MS
Juvekar
Aarti
A
Sen
Subrata
S
Zingde
Surekha
S
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
D000970:Antineoplastic Agents; D001581:Benzothiadiazines; D007202:Indicators and Reagents; D001569:Benzodiazepines; D004247:DNA; D004262:DNA Restriction Enzymes