title: Design and synthesis of novel hydroxyalkylaminomethylchromones for their IL-5 inhibitory activity.
abstract: A series of hydroxyalkylaminomethylchromone analogs 3 were prepared and evaluated as inhibitors of interleukin-5. The most active analog 3d inhibited interleukin-5 activity with an IC₅₀ of 17.5 μM. The structural requirements of chromone analogs possessing the inhibitory activity against IL-5 could be summarized as: (i) the cyclohexylmethoxy group at 5th position of the A ring, (ii) the planarity of chromone ring, (iii) hydrophobic unit around the B ring with hydroxyl functional group, (iv) the hydrophobic unit which does not have to be a planar and (v) the length of carbon units between amino and hydroxyl group is limited to two.
authors.affiliation: College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, Daejeon 305-764, Republic of Korea.
authors.forename: P
authors.initials: P
authors.lastname: Thanigaimalai
authors.forename: Ki-Cheul
authors.initials: KC
authors.lastname: Lee
authors.forename: Vinay K
authors.initials: VK
authors.lastname: Sharma
authors.forename: Jun-Ho
authors.initials: JH
authors.lastname: Yun
authors.forename: Youngsoo
authors.initials: Y
authors.lastname: Kim
authors.forename: Sang-Hun
authors.initials: SH
authors.lastname: Jung
mesh_terms: D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002460:Cell Line; D002867:Chromones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D015195:Drug Design; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D015848:Interleukin-5 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: C559232:3-((1-cyclohexyl-3-hydroxypropan-2-ylamino)methyl)-5-(cyclohexylmethoxy)-4H-chromen-4-one; D000893:Anti-Inflammatory Agents; D002867:Chromones; D015848:Interleukin-5