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Benzo[b]furan derivatives induces apoptosis by targeting the PI3K/Akt/mTOR signaling pathway in human breast cancer cells.
Bioorg Chem. 2016 06; 66:124-31.BC

Abstract

The PI3K/Akt/mTOR signaling pathway plays a key regulatory function in cell survival, proliferation, migration, metabolism and apoptosis. Aberrant activation of the PI3K/Akt/mTOR pathway is found in many types of cancer and thus plays a major role in breast cancer cell proliferation. In our previous studies, benzo[b]furan derivatives were evaluated for their anticancer activity and the lead compounds identified were 26 and 36. These observations prompted us to investigate the molecular mechanism and apoptotic pathway of these lead molecules against breast cancer cells. Benzo[b]furan derivatives (26 and 36) were evaluated for their antiproliferative activity against human breast cancer cell lines MCF-7 and MDA MB-231. These compounds (26 and 36) have shown potent efficiency against breast cancer cells (MCF-7) with IC50 values 0.057 and 0.051μM respectively. Cell cycle analysis revealed that these compounds induced cell cycle arrest at G2/M phase in MCF-7 cells. Western blot analysis revealed that these compounds inhibit the PI3K/Akt/mTOR signaling pathway and induced mitochondrial mediated apoptosis in human breast cancer cells (MCF-7).

Authors+Show Affiliations

Medicinal Chemistry and Pharmacology, CSIR - Indian Institute of Chemical Technology, Hyderabad 500 007, India; Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research, Hyderabad 500 037, India. Electronic address: ahmedkamal@iict.res.in.Medicinal Chemistry and Pharmacology, CSIR - Indian Institute of Chemical Technology, Hyderabad 500 007, India.CSIR-Centre for Cellular and Molecular Biology, Uppal Road, Hyderabad 500 007, India.Medicinal Chemistry and Pharmacology, CSIR - Indian Institute of Chemical Technology, Hyderabad 500 007, India.Medicinal Chemistry and Pharmacology, CSIR - Indian Institute of Chemical Technology, Hyderabad 500 007, India.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

27149364

Citation

Kamal, Ahmed, et al. "Benzo[b]furan Derivatives Induces Apoptosis By Targeting the PI3K/Akt/mTOR Signaling Pathway in Human Breast Cancer Cells." Bioorganic Chemistry, vol. 66, 2016, pp. 124-31.
Kamal A, Lakshma Nayak V, Nagesh N, et al. Benzo[b]furan derivatives induces apoptosis by targeting the PI3K/Akt/mTOR signaling pathway in human breast cancer cells. Bioorg Chem. 2016;66:124-31.
Kamal, A., Lakshma Nayak, V., Nagesh, N., Vishnuvardhan, M. V., & Subba Reddy, N. V. (2016). Benzo[b]furan derivatives induces apoptosis by targeting the PI3K/Akt/mTOR signaling pathway in human breast cancer cells. Bioorganic Chemistry, 66, 124-31. https://doi.org/10.1016/j.bioorg.2016.04.004
Kamal A, et al. Benzo[b]furan Derivatives Induces Apoptosis By Targeting the PI3K/Akt/mTOR Signaling Pathway in Human Breast Cancer Cells. Bioorg Chem. 2016;66:124-31. PubMed PMID: 27149364.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Benzo[b]furan derivatives induces apoptosis by targeting the PI3K/Akt/mTOR signaling pathway in human breast cancer cells. AU - Kamal,Ahmed, AU - Lakshma Nayak,V, AU - Nagesh,Narayana, AU - Vishnuvardhan,M V P S, AU - Subba Reddy,N V, Y1 - 2016/04/26/ PY - 2016/02/03/received PY - 2016/04/13/revised PY - 2016/04/25/accepted PY - 2016/5/6/entrez PY - 2016/5/6/pubmed PY - 2017/6/7/medline KW - Apoptosis KW - Benzo[b]furan derivatives KW - Breast cancer KW - Cell cycle KW - PI3K/Akt/mTOR pathway SP - 124 EP - 31 JF - Bioorganic chemistry JO - Bioorg Chem VL - 66 N2 - The PI3K/Akt/mTOR signaling pathway plays a key regulatory function in cell survival, proliferation, migration, metabolism and apoptosis. Aberrant activation of the PI3K/Akt/mTOR pathway is found in many types of cancer and thus plays a major role in breast cancer cell proliferation. In our previous studies, benzo[b]furan derivatives were evaluated for their anticancer activity and the lead compounds identified were 26 and 36. These observations prompted us to investigate the molecular mechanism and apoptotic pathway of these lead molecules against breast cancer cells. Benzo[b]furan derivatives (26 and 36) were evaluated for their antiproliferative activity against human breast cancer cell lines MCF-7 and MDA MB-231. These compounds (26 and 36) have shown potent efficiency against breast cancer cells (MCF-7) with IC50 values 0.057 and 0.051μM respectively. Cell cycle analysis revealed that these compounds induced cell cycle arrest at G2/M phase in MCF-7 cells. Western blot analysis revealed that these compounds inhibit the PI3K/Akt/mTOR signaling pathway and induced mitochondrial mediated apoptosis in human breast cancer cells (MCF-7). SN - 1090-2120 UR - https://www.unboundmedicine.com/medline/citation/27149364/Benzo[b]furan_derivatives_induces_apoptosis_by_targeting_the_PI3K/Akt/mTOR_signaling_pathway_in_human_breast_cancer_cells_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0045-2068(16)30036-0 DB - PRIME DP - Unbound Medicine ER -