Open AccessSynthesis and biological evaluation of 6H-1-benzopyrano[4,3-b]quinolin-6-one derivatives as inhibitors of colon cancer cell growth
Author(s) -
Tieling Li,
Haifeng Guo,
Fujuan Li,
Zhiguo Sun,
Hengchun Zhang
Publication year - 2015
Publication title -
bangladesh journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.385
H-Index - 23
eISSN - 1991-0088
pISSN - 1991-007X
DOI - 10.3329/bjp.v10i3.23645
Subject(s) - cytotoxicity , apoptosis , cytotoxic t cell , chemistry , dna fragmentation , colorectal cancer , cell culture , cancer cell , abcg2 , cell growth , cancer research , growth inhibition , microbiology and biotechnology , biochemistry , pharmacology , programmed cell death , cancer , transporter , biology , atp binding cassette transporter , in vitro , medicine , gene , genetics
A convenient synthesis of 6H-1-benzopyrano[4,3-b]quinolin-6-one derivatives was reported using 4-chloro-2-oxo-2H-chromene-3-carbaldehyde with different aromatic amines using silica sulfuric acid. The compounds were tested for their anticancer activity against colon (HCT-116 and S1-MI-80), prostate (PC3 and DU-145), breast (MCF-7 and MDAMB-231) cancer cells. These com-pounds showed more selectivity and potent cytotoxic activity against colon cancer cells. 3c was tested against five other colon cancer cell lines (HT-29, HCT-15, LS-180, LS-174, and LoVo), which had similar cytotoxicity and selectivity. 3c did not induce PXR-regulated ABCB1 or ABCG2 transporters. In fact, 3c induced cytotoxicity in HEK293 cells over expressing ABCB1 or ABCG2 to the same extent as in normal HEK293 cells. It was cytotoxic approximately 3- and 5-fold to resistant colon carcinoma S1-MI-80 cells. 3c also produced concentration-dependent changes in HCT-116 colon cancer cells, in mitochondrial membrane potential, leading to apoptosis, and sub-micromolar concentrations caused chromosomal DNA fragmentation