Specific stabilization of DNA triple helices by indolo[2,1-b]quinazolin-6,12-dione derivatives.
Derivatives of indolo[2,1-b]quinazolinone containing aminoalkylamino side chains were synthesized as specific DNA triplex stabilizing agents. The aminoalkylamino side chains are essential for triplex stabilization. The position-8 fluorine atom or a methyl group to the nitrogen adjacent to the planar core can enhance triplex stability by 6 degrees C and the effect is additive. Conformational analysis reveals that the orientation of the side chain underlies the ability of this compound to stabilize a DNA triplex.
Chen
Grace Shiahuy
GS
Department of Applied Chemistry, Providence University, Sha-Lu 43301, Taiwan, ROC.
Bhagwat
Bhalchandra V
BV
Liao
Pei-Yin
PY
Chen
Hui-Ting
HT
Lin
Shwu-Bin
SB
Chern
Ji-Wang
JW
D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002942:Circular Dichroism; D004247:DNA / Q000737:chemistry* / Q000187:drug effects*; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D008024:Ligands; D009690:Nucleic Acid Conformation / Q000187:drug effects; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013056:Spectrophotometry, Ultraviolet
D007211:Indoles; D008024:Ligands; D011799:Quinazolines; C046243:tryptanthrine; D004247:DNA