DOCKING STUDIES, SYNTHESIS, CHARACTERAZATION OF SOME NOVEL ISOXAZOLE
SUBSTITUTED 9-ANILINOACRIDINE DERIVATIVES AND EVALUATION FOR THEIR ANTI
TUMOR ACTIVITIES AS TOPO ISOMERASE II INHIBITORS
R. Kalirajan, S. Sankar, S. Jubie and B. Suresh
Department of Pharmaceutical Chemistry, JSS College of Pharmacy, (A Constituent college of JSS
University, Mysore), Udhagamandalam – 643001 (Tamilnadu), India
Abstract:
A series of some novel isoxazole substituted 9-anilinoacridines were synthesized to evaluate for their antitumor activity. It was revealed that these compounds exhibited significant antitumor activities. The docking studies of the synthesized compounds were performed towards the key Topoisomerase-II (1ZXM) by using Schrodinger Maestro 9.2 version. The isoxazole substituted 9-anilino acridine derivatives 5a-h have good docking scores against topo isomerise II compared with standard. The anti tumor activity was performed against Daltons Lymphoma Ascites (DLA) cell growth by in-vitro and in-vivo methods. The compounds 5c, 5e, 5f have significant anti tumor activity with CTC50 value of 235-275 µg/ml.
