benzofurans and fosbretabulin

benzofurans has been researched along with fosbretabulin* in 2 studies

Other Studies

2 other study(ies) available for benzofurans and fosbretabulin

Article	Year
Rapid induction of apoptosis in chronic lymphocytic leukemia cells by the microtubule disrupting agent BNC105. Cancer biology & therapy, 2016, Volume: 17, Issue:3 Microtubule targeting agents, such as vinblastine, are usually thought to arrest cells in mitosis and subsequently induce apoptosis. However, they can also cause rapid induction of apoptosis in a cell-cycle phase independent manner. BNC105 is a novel vascular and microtubule disrupting drug that also induces apoptosis rapidly but with markedly increased potency compared to vinca alkaloids and combretastatin A4. BNC105 binds to the colchicine-binding site on tubulin resulting in activation of c-Jun N-terminal kinase (JNK), phosphorylation of ATF2, and induction of ATF3 and Noxa leading to acute apoptosis in chronic lymphocytic leukemia (CLL) cells. Apoptosis induced by BNC105 is dependent upon both JNK activation and Noxa induction. Normal leukocytes and one CLL sample also exhibited JNK activation but not Noxa induction and were resistant to BNC105. This study emphasizes the importance of Noxa and JNK for induction of apoptosis in CLL cells by microtubule targeting drugs, and highlights the potential of BNC105 as a potent therapeutic to treat haematopoietic malignancies. Topics: Anisoles; Apoptosis; Benzofurans; Cell Line, Tumor; Humans; JNK Mitogen-Activated Protein Kinases; Leukemia, Lymphocytic, Chronic, B-Cell; MAP Kinase Signaling System; Microtubules; Stilbenes; Transfection; Tubulin Modulators; Vinblastine	2016
Synthesis and biological evaluation of novel heterocyclic derivatives of combretastatin A-4. Bioorganic & medicinal chemistry letters, 2012, Dec-01, Volume: 22, Issue:23 A novel series of combretastatin A-4 heterocyclic analogues was prepared by replacement of the B ring with indole, benzofurane or benzothiophene, attached at the C2 position. These compounds were evaluated for their abilities to inhibit tubulin assembly: derivative cis3b, having a benzothiophene, showed an activity similar to those of colchicine or deoxypodophyllotoxine. The antiproliferative and antimitotic properties of cis3b against keratinocyte cancer cell lines were also evaluated and the intracellular organization of microtubules in the cells after treatment with both stereoisomers of 3b was also determined, using confocal microscopy. Topics: Antimitotic Agents; Benzofurans; Cell Cycle Checkpoints; Cell Line, Tumor; Cell Proliferation; Colchicine; Heterocyclic Compounds; Humans; Indoles; Microscopy, Confocal; Microtubules; Stereoisomerism; Stilbenes; Thiophenes	2012

Article

Year

Rapid induction of apoptosis in chronic lymphocytic leukemia cells by the microtubule disrupting agent BNC105.

Cancer biology & therapy, 2016, Volume: 17, Issue:3

Microtubule targeting agents, such as vinblastine, are usually thought to arrest cells in mitosis and subsequently induce apoptosis. However, they can also cause rapid induction of apoptosis in a cell-cycle phase independent manner. BNC105 is a novel vascular and microtubule disrupting drug that also induces apoptosis rapidly but with markedly increased potency compared to vinca alkaloids and combretastatin A4. BNC105 binds to the colchicine-binding site on tubulin resulting in activation of c-Jun N-terminal kinase (JNK), phosphorylation of ATF2, and induction of ATF3 and Noxa leading to acute apoptosis in chronic lymphocytic leukemia (CLL) cells. Apoptosis induced by BNC105 is dependent upon both JNK activation and Noxa induction. Normal leukocytes and one CLL sample also exhibited JNK activation but not Noxa induction and were resistant to BNC105. This study emphasizes the importance of Noxa and JNK for induction of apoptosis in CLL cells by microtubule targeting drugs, and highlights the potential of BNC105 as a potent therapeutic to treat haematopoietic malignancies.

Topics: Anisoles; Apoptosis; Benzofurans; Cell Line, Tumor; Humans; JNK Mitogen-Activated Protein Kinases; Leukemia, Lymphocytic, Chronic, B-Cell; MAP Kinase Signaling System; Microtubules; Stilbenes; Transfection; Tubulin Modulators; Vinblastine

2016

Synthesis and biological evaluation of novel heterocyclic derivatives of combretastatin A-4.

Bioorganic & medicinal chemistry letters, 2012, Dec-01, Volume: 22, Issue:23

A novel series of combretastatin A-4 heterocyclic analogues was prepared by replacement of the B ring with indole, benzofurane or benzothiophene, attached at the C2 position. These compounds were evaluated for their abilities to inhibit tubulin assembly: derivative cis3b, having a benzothiophene, showed an activity similar to those of colchicine or deoxypodophyllotoxine. The antiproliferative and antimitotic properties of cis3b against keratinocyte cancer cell lines were also evaluated and the intracellular organization of microtubules in the cells after treatment with both stereoisomers of 3b was also determined, using confocal microscopy.

Topics: Antimitotic Agents; Benzofurans; Cell Cycle Checkpoints; Cell Line, Tumor; Cell Proliferation; Colchicine; Heterocyclic Compounds; Humans; Indoles; Microscopy, Confocal; Microtubules; Stereoisomerism; Stilbenes; Thiophenes

2012