The present invention pertains to certain N
8
,N
13
-disubstituted quino[4,3,2-kl]acridinium salts of formula (Q
−
) which inhibit telomerase wherein: p is an integer from 0 to 4; q is an integer from 0 to 3; r is an integer from 0 to 4; each R
A
is —H or a ring substituent; each R
B
is —H or a ring substituent; each R
C
is —H or a ring substituent; R
N8
is a nitrogen substituent; R
N13
is a nitrogen substituent; and, Q is an anion. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit telomerase, to regulate cell proliferation, and in the treatment of proliferative conditions, such as cancer.
本发明涉及一些具有式(Q-)的N8,N13-二取代喹诺[4,3,2-kl]
蒽盐,其抑制端粒酶,其中:p为0至4的整数;q为0至3的整数;r为0至4的整数;每个RA是—H或环取代基;每个RB是—H或环取代基;每个RC是—H或环取代基;RN8是一个氮取代基;RN13是一个氮取代基;而Q是一个阴离子。本发明还涉及包含这种化合物的制药组合物,以及这些化合物和组合物在体内外抑制端粒酶,调节细胞增殖以及治疗增生性疾病(如癌症)中的用途。