title: 4-Aminopyrimidines as novel HIV-1 inhibitors.
abstract: A series of 4-aminopyrimidines (1) was identified as novel HIV inhibitors of unknown molecular target. Structural modifications were carried out to establish its SAR and identify the linking site for target identification. A number of analogs were found to possess single digit inhibitory activity for HIV replication. Several analogs with various potential linkers, including a biotinated analog, also exhibited excellent potency, and could serve as tools for the identification of novel anti-HIV targets.
authors.affiliation: Genomics Institute of the Novartis Research Foundation (GNF), 10675 John Jay Hopkins Drive, San Diego, CA 92121, USA.
authors.forename: Venkat R
authors.initials: VR
authors.lastname: Gadhachanda
authors.forename: Baogen
authors.initials: B
authors.lastname: Wu
authors.forename: Zhiwei
authors.initials: Z
authors.lastname: Wang
authors.forename: Kelli L
authors.initials: KL
authors.lastname: Kuhen
authors.forename: Jeremy
authors.initials: J
authors.lastname: Caldwell
authors.forename: Helmut
authors.initials: H
authors.lastname: Zondler
authors.forename: Harald
authors.initials: H
authors.lastname: Walter
authors.forename: Mark
authors.initials: M
authors.lastname: Havenhand
authors.forename: Yun
authors.initials: Y
authors.lastname: He
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects*; D011743:Pyrimidines / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D019380:Anti-HIV Agents; D011743:Pyrimidines; C034821:4-aminopyrimidine