Opening book details…
Can I read Synthesis and structure-activity relationship study of 8-hydroxyquinoline-derived Mannich bases as anticancer agents on EtoBox?
Synthesis and structure-activity relationship study of 8-hydroxyquinoline-derived Mannich bases as anticancer agents by Arthur Y. Shaw; Chun-Yi Chang; Mei-Yuan Hsu; Pei-Jung Lu; Chia-Ning Yang; Hui-Ling Chen; Cheng-Wei Lo; Chung-Wai Shiau; Ming-Kai Chern is a Chemistry article available to read on EtoBox.
What is Synthesis and structure-activity relationship study of 8-hydroxyquinoline-derived Mannich bases as anticancer agents about?
To continue our early study on the structural modifications of clioquinol, more 8-hydroxyquinolinederived Mannich bases were synthesized and examined for growth-inhibitory effect. Taken Mannich base 1 as our lead compound, upon replacement of either sulfonyl group with methylene group or piperazine ring with ethylenediamine group resulted in an appreciable increase in potency. On the other hand, as 8-hydroxyquinoline was replaced with phenol, 3-hydroxypyridine and 1-naphthol, a dramatic decrease in activity was observed, indicating that 8-hydroxyquinoline is a crucial scaffold for activity. Further 3D-QSAR analysis on HeLa cells revealed that both steric and electronic effects contributed equally to growth inhibition. Taken together, the structure-activity relationships obtained from both in vitro data and CoMFA model warrant a valuable reference for further study.
Who reads Synthesis and structure-activity relationship study of 8-hydroxyquinoline-derived Mannich bases as anticancer agents?
It is typically read by researchers, students, and practitioners in Chemistry.
- Author
- Arthur Y. Shaw; Chun-Yi Chang; Mei-Yuan Hsu; Pei-Jung Lu; Chia-Ning Yang; Hui-Ling Chen; Cheng-Wei Lo; Chung-Wai Shiau; Ming-Kai Chern
- Publisher
- Elsevier Science; Elsevier ; Elsevier BV (ISSN 0223-5234)
- Published
- 2010
- Language
- EN
- Field
- Chemistry (Physical Sciences)