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Synthesis and in vitro anti-proliferative effects of 3-(hetero)aryl substituted 3-[(prop-2-ynyloxy)(thiophen-2-yl)methyl]pyridine derivatives on various cancer cell lines
Affiliation:1. Dr. Reddy’s Institute of Life Sciences, University of Hyderabad Campus, Hyderabad 500046, Andhra Pradesh, India;2. Department of Chemistry, Krishna University, Machilipatnam 521001, Andhra Pradesh, India;3. Department of Animal Sciences, School of Life Sciences, University of Hyderabad, Gachibowli, Hyderabad 500046, Andhra Pradesh, India;4. Department of Chemistry, K.L. University, Vaddeswaram, Guntur 522502, Andhra Pradesh, India;5. Department of Chemistry and the National Institute for Biotechnology in the Negev, Ben-Gurion University of the Negev, Be’er-Sheva 84105, Israel;6. Doctoral Programme in Experimental Biology and Biomedicine, Center for Neuroscience and Cell Biology, University of Coimbra, 3004-517 Coimbra, Portugal;1. Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, 130 Meilong Road, Shanghai 200237, PR China;2. Shanghai Research Center for Modernization of Traditional Chinese Medicine, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, PR China;1. LUT Energy, Lappeenranta University of Technology, Laitaatsillantie 3, Savonlinna 57170, Finland;2. Department of Material Science and Engineering, Boise State University, 1910 University Drive, Boise, ID 83725, USA;1. Department of Chemistry, New York University, New York, NY 10003, USA;2. Nanometics LLC, 111 Great Neck Rd, Suite 212, Great Neck, NY 11021, USA;3. Cancer Institute, New York University School of Medicine, 550 First Avenue, New York, NY 10016, USA;4. Department of Radiology, New York University School of Medicine, 550 First Avenue, New York, NY 10016, USA;1. School of Pharmaceutical and Chemical Engineering, Taizhou University, Taizhou 318000, Zhejiang, PR China;2. Zhejiang Hisoar Pharmaceutical Co., Ltd, Taizhou 318000, Zhejiang, PR China;3. College of Chemistry and Environmental Engineering, Yangtze University, Jingzhou 434020, Hubei, PR China;1. Division of Chemical Engineering, Nanomaterials Processing Research Center, Chonbuk National University, 567 Baekje-Daero, Deokjin-gu, Jeonju, Jeonbuk 561-756, Republic of Korea;2. Department of Chemistry, Kunsan National University, 558 Daehak-ro, Gunsan, Jeonbuk 573-701, Republic of Korea;1. IFOM-IEO Campus, Via Adamello 16, 20139 Milan, Italy;2. Department of Experimental Oncology, IEO, Via Adamello 16, 20139 Milan, Italy;3. Department of Health Sciences, University of Milan, 20133 Milan, Italy;4. Department of Biomedical Sciences and Engineering, University of Nova Gorica, Glavni Trg 9, SI-5261 Vipava, Slovenia
Abstract:A series of 3-(hetero)aryl substituted 3-[(prop-2-ynyloxy)(thiophen-2-yl)methyl]pyridine derivatives were designed as potential anticancer agents. These compounds were conveniently prepared by using Pd/C–Cu mediated Sonogashira type coupling as a key step. Many of these compounds were found to be promising when tested for their in vitro anti-proliferative properties against six cancer cell lines. All these compounds were found to be selective towards the growth inhibition of cancer cells with IC50 values in the range of 0.9–1.7 μM (against MDA-MB 231 and MCF7 cells), comparable to the known anticancer drug doxorubicin.
Keywords:Alkyne  Coupling  Pd/C  Cancer  Anti-proliferation
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