title: 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.
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.
authors: Dr. Reddy's Institute of Life Sciences, University of Hyderabad Campus, Hyderabad 500046, Andhra Pradesh, India.
authors: Upendar
authors: U
authors: Reddy Chamakura
authors: Department of Chemistry, Krishna University, Machilipatnam 521001, Andhra Pradesh, India.
authors: E
authors: E
authors: Sailaja
authors: Dr. Reddy's Institute of Life Sciences, University of Hyderabad Campus, Hyderabad 500046, Andhra Pradesh, India.
authors: Balakrishna
authors: B
authors: Dulla
authors: Department of Animal Sciences, School of Life Sciences, University of Hyderabad, Gachibowli, Hyderabad 500046, Andhra Pradesh, India.
authors: Arunasree M
authors: AM
authors: Kalle
authors: Department of Chemistry, K.L. University, Vaddeswaram, Guntur 522502, Andhra Pradesh, India.
authors: S
authors: S
authors: Bhavani
authors: Department of Chemistry and the National Institute for Biotechnology in the Negev, Ben-Gurion University of the Negev, Be'er-Sheva 84105, Israel.
authors: D
authors: D
authors: Rambabu
authors: Doctoral Programme in Experimental Biology and Biomedicine, Center for Neuroscience and Cell Biology, University of Coimbra, 3004-517 Coimbra, Portugal.
authors: Ravikumar
authors: R
authors: Kapavarapu
authors: Department of Chemistry, Krishna University, Machilipatnam 521001, Andhra Pradesh, India.
authors: M V Basaveswara
authors: MV
authors: Rao
authors: Dr. Reddy's Institute of Life Sciences, University of Hyderabad Campus, Hyderabad 500046, Andhra Pradesh, India. Electronic address: manojitpal@rediffmail.com.
authors: Manojit
authors: M
authors: Pal
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D001665:Binding Sites; D002244:Carbon / Q000737:chemistry; D002384:Catalysis; D020134:Catalytic Domain; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003300:Copper / Q000737:chemistry; D051357:Cyclin-Dependent Kinase 2 / Q000737:chemistry / Q000378:metabolism; D004354:Drug Screening Assays, Antitumor; D057809:HEK293 Cells; D006801:Humans; D061986:MCF-7 Cells; D062105:Molecular Docking Simulation; D010165:Palladium / Q000737:chemistry; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D011725:Pyridines; D013876:Thiophenes; D010165:Palladium; D002244:Carbon; D003300:Copper; D051357:Cyclin-Dependent Kinase 2
keywords: Alkyne; Anti-proliferation; Cancer; Coupling; Pd/C