Ananda Kumar, C. S. and Kavitha, C. V. and Vinaya, K. and Benaka Prasad, S. B. and Thimmegowda, N. R. and Chandrappa, S. and Raghavan, Sathees C. and Rangappa, K. S. (2009) Synthesis and in vitro cytotoxic evaluation of novel diazaspiro bicyclo hydantoin derivatives in human leukemia cells: a SAR study. INVESTIGATIONAL NEW DRUGS, 27 (4). pp. 327-337. ISSN 1573-0646
Full text not available from this repository. (Request a copy)Abstract
To study the structure activity relationship (SAR) on the cytotoxic activity and probe the structural requirement for the potent antitumor activity, a series of novel diazaspiro bicyclo hydantoin derivatives were designed and synthesized. Their structures were confirmed by H-1 NMR, LCMS and IR analyses. The antiproliferative effect of these compounds were determined against human leukemia, K562 (chronic myelogenous leukemia) and CEM (T-cell leukemia) cells using trypan blue and MTT assay, and the SAR associated with the position of N-terminal substituents in diazaspiro bicyclo hydantoin have also been discussed. It has been observed that these compounds displayed strong, moderate and weak cytotoxic activities. Interestingly, compounds having electron withdrawing groups at third and fourth position of the phenyl ring displayed selectively cytotoxic activities to both the cell lines tested with IC50 value lower than 50 mu M. In addition, the cytotoxic activities of the compounds 7(a-o) bearing the substituents at N-3 position of diazaspiro bicyclo hydantoin increases in the order alkene > ester > ether and plays an important role in determining their antitumor activities. The position and number of substituents in benzyl group attached to N-8 of diazaspiro bicyclo hydantoin nucleus interacted selectively with specific targets leading to the difference of biochemical and pharmacological effects.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | Diazaspiro bicyclo hydantoin; Cytotoxic activities; Trypan blue dye exclusion assay; MTT assay; Leukemia; SAR |
| Subjects: | D Physical Science > Physics |
| Divisions: | Department of > Physics |
| Depositing User: | Users 19 not found. |
| Date Deposited: | 20 Aug 2019 09:33 |
| Last Modified: | 11 Dec 2019 10:27 |
| URI: | http://eprints.uni-mysore.ac.in/id/eprint/6809 |
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