Editor-in-Chief Hatice Kübra Elçioğlu Vice Editors Levent Kabasakal Esra Tatar Online ISSN 2630-6344 Publisher Marmara University Frequency Bimonthly (Six issues / year) Abbreviation J.Res.Pharm. Former Name Marmara Pharmaceutical Journal
Marmara Pharmaceutical Journal 2013 , Vol 17 , Issue 2
Synthesis and chemotherapeutic activities of 5-chloro-1H-indole-2,3-dione 3-thiosemicarbazones
Görkem Ermut1, Nilgün Karalı1, İdil Çetin2, Mehmet Topçul3, Seher Birteksöz4
1Istanbul University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Istanbul, Turkey
2Istanbul University, Institute of Science, Department of Biology, Istanbul, Türkiye
3Istanbul University, Faculty of Science, Department of Biology, Istanbul, Turkey
4Istanbul University, Faculty of Pharmacy, Department of Pharmaceutical Microbiology, Istanbul, Turkey
DOI : 10.12991/201317383 A series of 5-chloro-1H-indole-2,3-dione 3-thiosemicarbazones 3a-g were synthesized to investigate the chemotherapeutic activities. The structures of 3a-g were confirmed by the spectral data (IR, 1H NMR, 13C NMR-APT, 13C NMR-DEPT, HSQC, HMBC) and elemental analysis. Anticancer activities of the compounds were evaluated using cell kinetic parameters on HeLa cells derived from human cervix carcinoma. The preliminary screening results indicated that alkyl substituted compounds 3a, 3b and 3d were more effective in mitosis phase when compared to the synthesis phase. 3a-g were tested against some DNA and RNA viruses in CRFK, HeLa, HEL, MDCK and Vero cells. None of the compounds was active against any of the RNA or DNA viruses at 100 μM. All compounds were also evaluated for antimicrobial activity against selected strains. Methyl substituted 3a and allyl substituted 3c were found to be active against S. aureus and C. albicans. Keywords : Anticancer activity, antiviral activity, antimicrobial activity, 5-chloro-1Hindole- 2,3-dione, thiosemicarbazone
Marmara University