Benaka Prasad, S. B. and Vinaya, K. and Ananda Kumar, C. S. and Sanjay Swarup and Rangappa, K. S. (2009) Synthesis of novel 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole derivatives as antiproliferative agents: A structure-activity relationship study. INVESTIGATIONAL NEW DRUGS, 27 (6). pp. 534-542. ISSN 0167-6997
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A series of novel 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole derivatives 5(a-m) were synthesized with different substituted aromatic/heterocyclic acid chlorides (R-CO-Cl) and characterized by H-1 NMR, LC/MS, FTIR and elemental analyses. All the compounds synthesised were evaluated for their antiproliferative activity by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. The antiproliferative effects of the synthesised compounds were tested against viable human skin fibroblast cells and carcinoma cells namely HeLa cells, HT-29 cells, MCF-7 cells, HepG-2 cells by adopting positive and negative control. The importance of the aromatic and heterocyclic moiety was confirmed. From the SAR studies, it reveals that, the substitution at N-terminal of 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole by the heterocyclic ring plays a dominant role and was responsible for the antiproliferative activity. Among the synthesized compounds 5a, 5d and 5k have showed potent antiproliferative activity on all the carcinoma cells tested.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | Isonipecotic acid; 6-fluoro-3-(4-piperidinyl)-1; 2-benzisoxazole; Acid chloride; MTT assay; Antiproliferative activity; Cancer therapy; Cell proliferation |
| Subjects: | C Chemical Science > Chemistry |
| Divisions: | Department of > Chemistry |
| Depositing User: | Users 19 not found. |
| Date Deposited: | 13 Aug 2019 05:32 |
| Last Modified: | 13 Aug 2019 05:32 |
| URI: | http://eprints.uni-mysore.ac.in/id/eprint/6305 |
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