Acridone-derived bisintercalators as chemotherapeutic agents

Details Acridone-derived bisintercalators as chemotherapeutic agents Acridone-derived bisintercalators as chemotherapeutic agents

C - Chemistry, Metallurgy

07

D

C07D 471/06 (2006.01) A61K 31/47 (2006.01) A61K 31/473 (2006.01) A61K 49/00 (2006.01) C07D 219/08 (2006.01) C07D 519/00 (2006.01) C07H 21/00 (2006.01) C12Q 1/68 (2006.01)

Patent

CA 2185350

The present invention provides a compound having structure (I), wherein R is - H, -CH3, or -C2H5; R1 and R2 are independently -H, -OH, -NH2, -OCH3, -C(CH3)3, or a halogen atom; n is 2 to 6; X and X' are independently -N or -NO2; Y and Y' are independently -N, -CH, or -H; and the double-slash represents a double bond or no bond; such that when X or X' is -N, Y or Y' is -CH or -N, and the double-slash is a double bond, and when X or X' is -NO2, Y or Y' is -H, and the double-slash is no bond. The present invention also provides a pharmaceutical composition comprising the compound above and a pharmaceutically acceptable carrier. The present invention further provides a method for treating a neoplastic cell growth in a subject in need of such treatment which comprises administering to the subject an amount of the pharmaceutical composition above effective to treat the neoplastic cell growth. Lastly, the present invention provides nucleic acid labeled with the compound above, as well as a method for detecting nucleic acid in a sample.

L'invention concerne un composé possédant la structure (I) dans laquelle R représente -H, -CH¿3? ou -C¿2?H¿5?; R1 et R2 représentent indépendamment -H, -OH, -NH¿2?, -OCH¿3?, -C(CH¿3?)¿3? ou un atome d'halogène; n représente 2 à 6; X et X' représentent indépendamment -N ou -NO¿2?; Y et Y' représentent indépendamment -N, -CH ou -H et la double barre oblique représente une liaison double ou l'absence de liaison, de telle manière que, quand X ou X' représente -N, Y ou Y' représente -CH ou -N et la double barre oblique représente une liaison double, et quand X ou X' représente -NO¿2?, Y ou Y' représente -H et la double barre oblique représente l'absence de liaison. L'invention concerne également une composition pharmaceutique comprenant ledit composé et un excipient pharmaceutiquement acceptable. Elle concerne encore un procédé de traitement d'une croissance cellulaire néoplasique chez un patient qui consiste à administrer une dose efficace de ladite composition audit patient, afin de traiter ladite croissance cellulaire. Elle concerne enfin un acide nucléique marqué au moyen dudit composé, ainsi qu'un procédé de détection d'acide nucléique dans un échantillon.

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