Tandon, Vishnu K. ; Maurya, Hardesh K. ; Tripathi, Ashutosh ; ShivaKeshava, G. B. ; Shukla, Praveen K. ; Srivastava, Pallavi ; Panda, Dulal (2009) 2,3-Disubstituted-1,4-naphthoquinones, 12H-benzo[b]phenothiazine-6,11-diones and related compounds: synthesis and biological evaluation as potential antiproliferative and antifungal agents European Journal of Medicinal Chemistry, 44 (3). pp. 1086-1092. ISSN 0223-5234
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Official URL: http://linkinghub.elsevier.com/retrieve/pii/S02235...
Related URL: http://dx.doi.org/10.1016/j.ejmech.2008.06.025
Abstract
A series of 2-chloro-3-arylsulfanyl-[1,4]naphthoquinones (2), 2,3-bis-arylsulfanyl-[1,4]naphthoquinones (3) and 12H-benzo[b]phenothiazine-6,11-diones and their analogs 6-8 were synthesized and evaluated for their antiproliferative activity against human cervical cancer (HeLa) cells. Compounds 3a and 3b were found to possess most potent antiproliferative and cell killing ability. Compounds 1-8 were also evaluated for antifungal activities. The structure–activity relationship of these compounds was studied and the results show that compound 2a (MIC50=1.56μg/mL) exhibited in vitro potent antifungal activity compared to the clinically useful antifungal drug Fluconazole (MIC50=2.0 μg/mL) against Sporothrix. schenckii. Compound 2a (MIC50=1.56μg/mL) also exhibited same antifungal activity compared to clinically useful drug Amphotericin-B (MIC50=1.56μg/mL) against Trichophyton. mentagraphytes.
| Item Type: | Article |
|---|---|
| Source: | Copyright of this article belongs to Elsevier Science. |
| Keywords: | Antiproliferative; 1,4-Naphthoquinone Derivatives; Cytotoxic; Human Cervical Cancer (HeLa) Cells; Antifungal |
| ID Code: | 34932 |
| Deposited On: | 14 Apr 2011 13:54 |
| Last Modified: | 14 Apr 2011 13:54 |
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