Synthesis and Anticancer Activity of Some Novel Tolmetin Thiosemicarbazides

Dadas Y., Coskun G. P., Bingol-Akpinar O., ÖZSAVCI D., KÜÇÜKGÜZEL Ş. G.

MARMARA PHARMACEUTICAL JOURNAL, cilt.19, sa.3, ss.259-267, 2015 (ESCI) identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 19 Sayı: 3
  • Basım Tarihi: 2015
  • Doi Numarası: 10.12991/mpj.201519328306
  • Dergi Adı: MARMARA PHARMACEUTICAL JOURNAL
  • Derginin Tarandığı İndeksler: Emerging Sources Citation Index (ESCI), TR DİZİN (ULAKBİM)
  • Sayfa Sayıları: ss.259-267
  • Anahtar Kelimeler: Apoptosis, tolmetin, thiosemicarbazide, PC-3, colon cancer, ANTIMICROBIAL ACTIVITY, BIOLOGICAL EVALUATION, CANCER, MATRIX, DERIVATIVES, CELLS
  • Marmara Üniversitesi Adresli: Evet

Özet

A novel series of new ten tolmetin hydrazide derivatives, N-Alkyl/Arylsubstituted-2-{[1-methyl-5-(4-methylbenzoyl)-1H- pyrrol-2-yl]acetyl}hydrazinecarbothioamides [4a-j] have been synthesized in this study. The structures of the new compounds were determined by spectral (FT-IR, H-1-NMR, C-13-NMR and 2D-NMR) methods and their purity were proven by elemental analysis and TLC. Tolmetin [1] and N-(4-fluorophenyl)-2-{[1-methyl-5-(4-methylbenzoyl)-1H-pyrrol-2- yl] acetyl}hydrazinecarbothioamide [4d] were evaluated for in vitro using the MTT colorimetric method for anticancer activity. Androjen-independed human prostate cancer cell line PC-3 (ATCC, CRL-1435), human colon cancer cell lines HCT-116 (ATCC, CCL-247) and HT-29 (ATCC, HTB-38) were used in this study. Compound 4d exhibited anticancer activity against PC-3 whereas Tolmetin showed minor activity comparing to compound 4d.