Pentafluorophenyl substitution of natural di(indol-3-yl)methane strongly enhances growth inhibition and apoptosis induction in various cancer cell lines.

Pentafluorophenyl substitution of natural di(indol-3-yl)methane strongly enhances growth inhibition and apoptosis induction in various cancer cell lines.
Chem Biodivers. 2019 Feb 04;:
Authors: Ahmad A, Dandawate P, Schruefer S, Padhye S, Sarkar FH, Schobert R, Biersack B
Abstract
Di(indol-3-yl)methane (DIM, 1) is a known weakly antitumoral compound formed by digestion of indole-3-carbinol, an ingredient of various Brassica vegetables. Out of a series of nine fluoroaryl derivatives of 1, three pentafluorophenyl derivatives 2c, 2h and 2i were identified that exhibited a two to five times greater anti-proliferative effect and an increased apoptosis induction when compared with 1 in the following carcinoma cell lines: BxPC-3 pancreas, LNCaP prostate, C4-2B prostate, PC3 prostate and the triple-negative MDA-MB-231 breast carcinoma. Compound 2h was particularly efficacious against androgen-refractory C4-2B prostate cancer cells (IC50 = 6.4 µM) and 2i against androgen-responsive LNCaP cells (IC50 = 6.2 µM). In addition, 2c and 2h exhibited distinct activity in three cancer cell lines resistant to 1.
PMID: 30715794 [PubMed - as supplied by publisher]

Source: Chemistry and Biodiversity - February 4, 2019 Category: Biochemistry Authors: Ahmad A, Dandawate P, Schruefer S, Padhye S, Sarkar FH, Schobert R, Biersack B Tags: Chem Biodivers Source Type: research