title: Facile Diversity-Oriented Synthesis of Polycyclic Pyridines and Their Cytotoxicity Effects in Human Cancer Cell Lines.
abstract: A three-component cascade method has been developed for the direct synthesis of polysubstituted pyridines. This strategy provides a very convenient route to pyridines using a variety of β-bromo-α,β-unsaturated aldehydes, 1,3-diketones, and ammonium acetate without any additional catalyst or metal salt under mild conditions. A variety of β-ketoesters and 4-hydroxycoumarin were also used instead of 1,3-diketones for the diverse synthesis of polycyclic pyridines. One of the synthesized pyridines has been unambiguously established by a single crystal XRD study. All of the synthesized pyridine derivatives were evaluated for their antiproliferative properties in vitro against the human cancer cell lines HeLa, Me180, and ZR751. Compounds 4{4,1} and 4{2,4} showed significant cytotoxicity in the human breast cancer cell line ZR751 and cervical cancer cell line Me180, respectively, and a few other compounds were found to have moderate activities.
authors.affiliation: Medicinal Chemistry Division and ‡Analytical Chemistry Division, CSIR-North East Institute of Science and Technology , Jorhat, Assam 785006, India.
authors.forename: Limi
authors.initials: L
authors.lastname: Goswami
authors.affiliation: Medicinal Chemistry Division and ‡Analytical Chemistry Division, CSIR-North East Institute of Science and Technology , Jorhat, Assam 785006, India.
authors.forename: Shyamalee
authors.initials: S
authors.lastname: Gogoi
authors.affiliation: Medicinal Chemistry Division and ‡Analytical Chemistry Division, CSIR-North East Institute of Science and Technology , Jorhat, Assam 785006, India.
authors.forename: Junali
authors.initials: J
authors.lastname: Gogoi
authors.affiliation: Medicinal Chemistry Division and ‡Analytical Chemistry Division, CSIR-North East Institute of Science and Technology , Jorhat, Assam 785006, India.
authors.forename: Rajani K
authors.initials: RK
authors.lastname: Boruah
authors.affiliation: Medicinal Chemistry Division and ‡Analytical Chemistry Division, CSIR-North East Institute of Science and Technology , Jorhat, Assam 785006, India.
authors.forename: Romesh C
authors.initials: RC
authors.lastname: Boruah
authors.affiliation: Medicinal Chemistry Division and ‡Analytical Chemistry Division, CSIR-North East Institute of Science and Technology , Jorhat, Assam 785006, India.
authors.forename: Pranjal
authors.initials: P
authors.lastname: Gogoi
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001943:Breast Neoplasms / Q000188:drug therapy / Q000473:pathology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003603:Cytotoxins / Q000737:chemistry / Q000494:pharmacology; D005260:Female; D006801:Humans; D011083:Polycyclic Compounds / Q000138:chemical synthesis / Q000494:pharmacology; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology; D002583:Uterine Cervical Neoplasms / Q000188:drug therapy / Q000473:pathology
chemical_list: D000970:Antineoplastic Agents; D003603:Cytotoxins; D011083:Polycyclic Compounds; D011725:Pyridines
keywords: antitumor activity; cascade reaction; halovinyl aldehyde; pyridine