Laboratory of Immunogenetics, CSIR - Institute of Genomics and Integrative Biology, Delhi University Campus, Delhi, India.
Arch Pharm (Weinheim). 2012 May;345(5):368-77. doi: 10.1002/ardp.201100279. Epub 2011 Dec 20.
The interaction between leukocytes and the vascular endothelial cells (EC) via cellular adhesion molecules plays an important role in the pathogenesis of various inflammatory and autoimmune diseases. Small molecules that block these interactions have been targeted as potential therapeutic agents against acute and chronic inflammatory diseases. In an effort to identify potent intercellular cell adhesion molecule-1 (ICAM-1) inhibitors, a large number of arylalkyl ketones, benzophenones, desoxybenzoins and chalcones and their analogs (54 in total) have been synthesized and screened for their ICAM-1 inhibitory activity. The structure-activity relationship studies of these compounds identified three potent chalcone derivatives and also demonstrated the possible mechanism for their ICAM-1 inhibitory activities. The most active compound was found to be 79.
白细胞与血管内皮细胞（EC）通过细胞黏附分子的相互作用在各种炎症和自身免疫性疾病的发病机制中起着重要作用。阻断这些相互作用的小分子已被作为针对急性和慢性炎症性疾病的潜在治疗药物。为了鉴定有效的细胞间黏附分子-1（ICAM-1）抑制剂，已经合成了大量的芳基烷基酮、二苯甲酮、去氧苯并酮和查尔酮及其类似物（共 54 种），并对它们的 ICAM-1 抑制活性进行了筛选。这些化合物的构效关系研究鉴定出了三个有效的查尔酮衍生物，并还证明了它们抑制 ICAM-1 活性的可能机制。发现最活性的化合物是 79。
