SYNTHESIS AND ANTIPROLIFERATIVE ACTIVITY OF NEW INDOLOQUINOLINE – BIOTIN HYBRIDS

Elkhabiry Shaban*, Samah El-Ghlban, Marwa Samy, Ahmed Abdel Aleem El-Gokha and Ibrahim El-Tantawy El Sayed*

ABSTRACT

A series of indoloquinoline- biotin hybrids conjugates 7a-f were designed and synthesized in good yields to improve and develop higher potency and selective anti-tumor agents. Their antiproliferative evaluation activities against HePG2, HCT-116 and MCF-7 cell lines in vitro were tested using colorimetric MTT assay. These neocryptolepines (2-substituted-5-methyl-indolo[2,3-b]quinolones) were synthesized via nucleophilic aromatic substitution (SNAr) of the Cl leaving group of 11-chloroneocryptolepines with diamines which further hybrids by reacting the 11-(aminoalkylamino) derivatives with biotin. The result of the present work indicated also that 7e, 7f were good potent compared with doxorubicin and ultimately would be appreciated as potential anticancer agents.

Keywords: Chloroneocryptolepine, Biotin, aminoalkylamino-substituted, antiproliferative activity, doxorubicin.