Inventi Rapid: Med Chem

Inventi:prmc/10833/21

QSAR STUDIES OF N1-(ACRIDIN-9-YL) BENZENE-1,3-DIAMINE DERIVATIVES AS POTENT ANTICANCER AGENTS AGAINST TSGH CANCER CELL LINE

N1-(Acridin-9-yl) Benzene-1,3-Diaminederivative having potent anticancer activity. The anticancer effect of N1-(Acridin-9-yl) Benzene-1, 3-Diamine analogues is on the Gastric carcinoma TSGH, Human adenocarcinoma [colon & rectal] tumor [HT-29] cell line, Human nasopharyngeal carcinoma [HONE-1] cell line & Human brain tumor [DBTRG] cell line & it�s significant cytotoxic activity against human leukemic HL-60 cell growth. The cytotoxic activity of the N1-(Acridin-9-yl) Benzene-1, 3-Diamine-alkylcarbamates is decreased with increasing length & size of the alkyl function. It�s having also drug�DNA binding affinity. These compound having higher cytotoxic activity due to high lipophilicity. We are using 26 compounds and those pIC50 activities on the three different cell lines; TSGH cell line for the 2-D QSAR study. Here the 2D-QSAR studies of N1-(Acridin-9-yl) Benzene-1, 3-Diamine analogues were performed by using software Chem-Draw Ultra-8.0, Openbable-2.2.1, Dragon, Valstat and Microsoft Excel-2010 for r2 value. We are considering here two model equations for QSAR study. The value of linearity for model-1 of TSGH was found to be r2= 0.857767, Q2= 0.810095, Spress= 0.345507 and SDEP= 0.31782 while for these value for model-2 r2= 0.848466, Q2= 0.79321, Spress= 0.36053 and SDEP= 0.33164. This both models of TSGH cell line activity was validated by the Valstat software....