DNA-directed alkylating agents: synthesis, antitumor activity and DNA affinity of bis-N,N'-trisubstituted 1,2,4-triazolo-piperazines.
A series of 1,4-bis-(1,5-dialkyl-1H-1,2,4-triazol-ylmethyl)piperazines and N-methyl-piperazine analogs were prepared spontaneously from the cycloaddition of various reactive cumulenes with the piperazino-1,4-(bis-ethanenitrile) and 1-cyanomethyl-4-methyl-piperazine, respectively. The new compounds were evaluated for their DNA affinity and antitumor activity.
Al-Soud
Yaseen A
YA
Department of Chemistry, College of Science, University of Al al-Bayt, 25113, Al-Mafraq, Jordan.
Al-Masoudi
Najim A
NA
D000818:Animals; D018906:Antineoplastic Agents, Alkylating / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002417:Cattle; D002455:Cell Division / Q000187:drug effects; D004247:DNA / Q000187:drug effects / Q000378:metabolism*; D004354:Drug Screening Assays, Antitumor; D015394:Molecular Structure; D010879:Piperazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D018906:Antineoplastic Agents, Alkylating; D010879:Piperazines; D004247:DNA; C427203:calf thymus DNA