Synthesis and primary cytotoxicity evaluation of new imidazo[2,1-b]thiazole derivatives
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, cilt.42, sa.3, ss.320-326, 2007 (SCI-Expanded, Scopus)
- Yayın Türü: Makale / Tam Makale
- Cilt numarası: 42 Sayı: 3
- Basım Tarihi: 2007
- Doi Numarası: 10.1016/j.ejmech.2006.10.012
- Dergi Adı: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
- Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
- Sayfa Sayıları: ss.320-326
- Anahtar Kelimeler: imidazo[2,1-b]thiazole, arylidenehydrazide, cytotoxicity, NATIONAL-CANCER-INSTITUTE, ANTI-TUMOR AGENTS, DRUG DISCOVERY, IMIDAZO<2,1-B>THIAZOLES
- İstanbul Üniversitesi Adresli: Evet
Özet
A series of arylidenehydrazides (3a-3i) were synthesized from [6-(4-bromophenyl)imidazo[2,1-b] thiazol-3-yl] acetic acid hydrazide. The structures of new compounds were determined by analytical and spectral (IR, H-1 NMR, C-13 NMR, EIMS) methods. The synthesized compounds (3a-3i) were evaluated in the National Cancer Institute's 3-cell line, one dose in vitro primary cytotoxicity assay. Compounds 3a-3c, 3h and 3i which passed the criteria for activity in this assay were scheduled automatically for evaluation against the full panel of 60 human tumour cell lines at a minimum of five concentrations at 10-fold dilutions. Compounds 3c demonstrated the most marked effects on a prostate cancer cell line (PC-3, log(10) GI(50) value < -8.00). (c) 2006 Elsevier Masson SAS. All rights reserved.