BIOLOGICAL EVALUATION OF BIS(INDOLYL)METHANE (BIM) DERIVATIVES AS BCL-2 INHIBITOR IN HL-60 CELLS

Indole has shown remarkable anticancer activities which resulted to exploration of compounds containing indole unit. 11 BIMs were synthesized and their antiproliferative activity against HL-60 cell were evaluated. Compounds 4 and 7 possess best potency of inhibition activity at concentration of 50 µM with IC50 values of 21.26 and 41.06 µM, respectively. UV-vis titration with ctDNA indicated the anticancer properties of BIM with the binding constant value (Kb) for 4 and 7 are 6.02×10⁴ M⁻¹ and 1.04×10⁴ M⁻¹ correspondingly. Ligands 4 and 7 exhibited good cytotoxicity activity. These bis-indolylmethanes possessed antiproliferative potential that can be scrutinized for future developments.