Synthesis and biological evaluation of new imidazo[2,1-b]thiazole derivatives as anticancer agents

Karaman B., Guzeldemirci N.

MEDICINAL CHEMISTRY RESEARCH, cilt.25, sa.11, ss.2471-2484, 2016 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 25 Sayı: 11
  • Basım Tarihi: 2016
  • Doi Numarası: 10.1007/s00044-016-1684-x
  • Dergi Adı: MEDICINAL CHEMISTRY RESEARCH
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.2471-2484
  • Anahtar Kelimeler: Anticancer activity, Imidazo[2, 1-b] thiazole, Arylidenehydrazide, NATIONAL-CANCER-INSTITUTE, HEPATOCELLULAR-CARCINOMA, ANTIMICROBIAL EVALUATION, ANTITUMOR-ACTIVITY, ADJUVANT THERAPY, DRUG DISCOVERY, TUMOR-CELLS, INHIBITORS, DESIGN, MECHANISMS
  • İstanbul Üniversitesi Adresli: Evet

Özet

A series of arylidenehydrazide compounds (3a-3j) were synthesized from [6-(4-chlorophenyl)imidazo[2,1-b]thiazol-3-yl]acetic acid hydrazide. The newly synthesized compounds 3b and 3h were subjected to the National Cancer Institute's in vitro disease-oriented antitumor screening to be evaluated for antitumor activity. Compound 3b, the most potent compound examined, displayed broad spectrum antiproliferative activity against all of the tested cell lines with log(10)GI(50) values between -4.41 and -6.44. The greatest growth inhibitions were observed against an ovarian cancer cell line(OVCAR-3), a colon cancer cell line (HCT-15), two renal cancer cell lines (CAKI-1 and UO-31) and two leukemia cell lines (CCRF-CEM and SR) with log(10)GI(10) values -6.44, -6.33, -6.11, -6.30, -6.13 and -6.22, respectively.