2-(1-Hydroxethyl)-4,8-dihydrobenzo[1,2-b:5,4-b']dithiophene-4,8-dione (BTP-11) enhances the ATRA-induced differentiation in human leukemia HL-60 cells.

  title={2-(1-Hydroxethyl)-4,8-dihydrobenzo[1,2-b:5,4-b']dithiophene-4,8-dione (BTP-11) enhances the ATRA-induced differentiation in human leukemia HL-60 cells.},
  author={Chun-Jen Chen and Yen-Fang Wen and Pi Tsan Huang and Mei-Hua Hsu and Kuo Hsiung Lee and Mei-Hwai Chen and Wuu-Chian Shin and Li‐Jiau Huang and Sheng-Chu Kuo},
  journal={Leukemia research},
  volume={33 12},
2-(1-Hydroxethyl)-4,8-dihydrobenzo[1,2-b:5,4-b']dithiophene-4,8-dione (BTP-11) is a potent enhancer for all-trans retinoic acid (ATRA)-induced differentiation in HL-60 cells. Combination of BTP-11 and ATRA cut down the concentration of ATRA significantly, and that BTP-11 promoted the progression of ATRA-induced into the terminal granulocytic differentiation. Further, Western blot analysis revealed that combination of BTP-11 and ATRA decreased cyclin D/CDK4 and increased C/EBPvarepsilon protein… Expand
3 Citations
Molecular mechanism of inhibitory effects of C-phycocyanin combined with all-trans-retinoic acid on the growth of HeLa cells in vitro
The C-PC + ATRA combination might take effect by inhibiting the progress of the cell cycle, inducing cell apoptosis and promoting complement-mediated cytolysis. Expand
The synergistic antitumor effects of all-trans retinoic acid and C-phycocyanin on the lung cancer A549 cells in vitro and in vivo.
Results showed both C-PC and ATRA could inhibit the growth of tumor cells in vivo and in vitro, and both ATRA+C-PC cooperatively showed a higher antitumor activity. Expand
Chlorogenic acid induced apoptosis and inhibition of proliferation in human acute promyelocytic leukemia HL‑60 cells.
The observations revealed that CA inhibits proliferation and induces preprophase apoptosis of HL‑60 cells, and the concentration of 10 µM may be the optimal dose for treatment human acute promyelocytic leukemia. Expand


Cell differentiation enhancement by hydrophilic derivatives of 4,8-dihydrobenzo[1,2-b:5,4-b']dithiophene-4,8-diones in HL-60 leukemia cells.
Two ester-type hydrophilic prodrugs are identified in this paper as new anti-leukemic drug candidates and exhibited excellent and equally potent differentiation effects on HL-60 cells. Expand
Synthesis and cytotoxicity of methyl-4,8-dihydrobenzo[1,2-b:5,4-b']dithiophene-4,8-dione derivatives.
2- and 3-Methyl-4,8-dihydrobenzo and related derivatives were synthesized and evaluated in vitro by NCI against eight cancer types and showed significant activity against melanoma, NCI-H23 non-small cell lung cancer, and MDA-MB-435 and Mda-N breast cancer cell lines. Expand
Synthesis and cytotoxicity of 2-acetyl-4,8-dihydrobenzodithiophene-4, 8-dione derivatives.
Compound 11, 2-(1'-acetoxyethyl)-4,8-dihydrobenzo[1,2-b:4,5-b']dithiophene-4, 8-dione, showed the highest overall potency (mean GI50 = 40 nM). Expand
1-(3,4-dimethoxyphenyl)-3,5-dodecenedione (I6) induces G1 arrest and apoptosis in human promyelocytic leukemia HL-60 cells.
I6 is a potent anti-HL-60 drug and possess a significant action on cell cycle before commitment for apoptosis occurrence, suggesting that the Bcl-2 expression decrease and caspase-3 activation may be the plausible mechanism by which I6 induced apoptosis. Expand
Synthesis of 1-substituted 3-pyridinylmethylidenylindolin-2-ones and 1-substituted 3-quinolinylmethylidenylindolin-2-ones as the enhancers of ATRA-induced differentiation in HL-60 cells.
The combination of 25 with all trans retinoic acid (ATRA) was found to induce complete differentiation of HL-60 cells and arrest the cells in the G(0)/G(1) phase of the cell cycle. Expand
1α,25-Dihydroxyvitamin D3–Induced Myeloid Cell Differentiation Is Regulated by a Vitamin D Receptor–Phosphatidylinositol 3-Kinase Signaling Complex
It is suggested that PI 3-kinase selectively regulates D3-induced monocyte differentiation, independent of any effects on p21, during maturation of myeloid cells and surface expressions of CD14 and CD11b. Expand
Combined effect of all-trans retinoic acid and arsenic trioxide in acute promyelocytic leukemia cells in vitro and in vivo.
Combined As(2)O(3) and tRA treatment may be more effective than single agents in tRA-resistant patients, and toxicity and potential drug antagonism may be diminished when given at the same time with therapeutic levels of tRA. Expand
Anticancer mechanisms of YC-1 in human lung cancer cell line, NCI-H226.
Findings suggest a mechanism of cytotoxic action of YC-1 and indicate that YC -1 may be a promising chemotherapy agent against lung cancer. Expand
Histone deacetylase inhibitors are the potent inducer/enhancer of differentiation in acute myeloid leukemia: a new approach to anti-leukemia therapy
HDRIs are the potent inducer or enhancer of differentiation in acute myeloid leukemia and regulate transcription in an ordered manner. Expand
Histone deacetylase inhibitor but not arsenic trioxide differentiates acute promyelocytic leukaemia cells with t(11;17) in combination with all‐trans retinoic acid
It is indicated that APL cells with t(11;17) need a higher concentration of ATRA than those with t[15;17] to differentiate and suggest that HDAC inhibitor is a promising differentiation enhancer in APL with t (11; 17). Expand