title: Identification and optimization of small molecule antagonists of vasoactive intestinal peptide receptor-1 (VIPR1).
abstract: Identification, synthesis and structure-activity relationship of small-molecule VIPR1 antagonists encompassing two chemical series are described.
authors.affiliation: Early Discovery Chemistry, Bristol-Myers Squibb Co., Princeton, NJ 08543-4000, USA. lalgudi.harikrishnan@bms.com
authors.forename: Lalgudi S
authors.initials: LS
authors.lastname: Harikrishnan
authors.forename: Neelam
authors.initials: N
authors.lastname: Srivastava
authors.forename: Lauren E
authors.initials: LE
authors.lastname: Kayser
authors.forename: David S
authors.initials: DS
authors.lastname: Nirschl
authors.forename: K
authors.initials: K
authors.lastname: Kumaragurubaran
authors.forename: Amrita
authors.initials: A
authors.lastname: Roy
authors.forename: Anuradha
authors.initials: A
authors.lastname: Gupta
authors.forename: Sukhen
authors.initials: S
authors.lastname: Karmakar
authors.forename: Tajudheen
authors.initials: T
authors.lastname: Karatt
authors.forename: Arvind
authors.initials: A
authors.lastname: Mathur
authors.forename: Neil T
authors.initials: NT
authors.lastname: Burford
authors.forename: Jing
authors.initials: J
authors.lastname: Chen
authors.forename: Yan
authors.initials: Y
authors.lastname: Kong
authors.forename: MaryEllen
authors.initials: M
authors.lastname: Cvijic
authors.forename: Christopher B
authors.initials: CB
authors.lastname: Cooper
authors.forename: Michael A
authors.initials: MA
authors.lastname: Poss
authors.forename: George L
authors.initials: GL
authors.lastname: Trainor
authors.forename: Tai W
authors.initials: TW
authors.lastname: Wong
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001713:Biphenyl Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D057166:High-Throughput Screening Assays; D006801:Humans; D051238:Receptors, Vasoactive Intestinal Polypeptide, Type I / Q000037:antagonists & inhibitors* / Q000378:metabolism; D054852:Small Molecule Libraries; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D001713:Biphenyl Compounds; D051238:Receptors, Vasoactive Intestinal Polypeptide, Type I; D054852:Small Molecule Libraries; D013876:Thiophenes