Effects of Immunomodulatory Derivatives of Thalidomide (IMiDs) and Their Analogs on Cell-Differentiation, Cyclooxygenase Activity and Angiogenesis

• Published in: Chemical & pharmaceutical bulletin Vol. 54; no. 6; pp. 855 - 860
• Main Authors: Fujimoto, Haruka, Noguchi, Tomomi, Kobayashi, Hisayoshi, Miyachi, Hiroyuki, Hashimoto, Yuichi
• Format: Journal Article
• Language: English
• Published: TOKYO The Pharmaceutical Society of Japan 01.06.2006; Pharmaceutical Soc Japan; Japan Science and Technology Agency
• Subjects: angiogenesis; Angiogenesis Inhibitors - pharmacology; Cell Differentiation - drug effects; Chemistry; Chemistry, Medicinal; Chemistry, Multidisciplinary; cyclooxygenase; Cyclooxygenase 1 - drug effects; differentiation; HL-60 Cells; Humans; Immunologic Factors - pharmacology; immunomodulatory derivative of thalidomide (IMiD); Life Sciences & Biomedicine; Pharmacology & Pharmacy; Physical Sciences; Science & Technology; thalidomide; Thalidomide - analogs & derivatives; Thalidomide - pharmacology; Tumor Cells, Cultured; Umbilical Veins - pathology; DRUG; differentiation; immunomodulatory derivative of thalidomide (IMiD); angiogenesis; FACTOR-ALPHA PRODUCTION; cyclooxygenase; LINES; COLON-CANCER; ANTIANGIOGENIC ACTIVITY; thalidomide; HL-60; INHIBITORS; ANTAGONISTS
• ISSN: 0009-2363; 1347-5223
• DOI: 10.1248/cpb.54.855

Various analogs of known immunomodulatory derivatives of thalidomide (1) (IMiDs: 3, 5) were synthesized, focusing on cell-differentiation-inducing, cyclooxygenase-inhibitory and anti-angiogenesis activities. Among the prepared compounds, NIDO-33 (14) showed cell differentiation-inducing activity on HL-60 cells and anti-angiogenic activity on human umbilical vein endothelial cells (HUVEC). AIDO-00 (7) also showed anti-angiogenic activity. NIDO-11 (8) showed an enhancing effect on all-trans retinoic acid (ATRA)-induced HL-60 cell differentiation, and AIDO-30 (13) exhibited cyclooxygenase (COX)-inhibitory activity.