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Synthesis and Antitumor Properties of 2,5-Bis(3'-indolyl) thiophenes: Analogues of Marine Alkaloid Nortopsentin
Synthesis and Antitumor Properties of 2,5-Bis(3'-indolyl) thiophenes: Analogues of Marine Alkaloid Nortopsentin
- Publication Year :
- 2007
- Publisher :
- Elsevier Science Limited, 2007.
-
Abstract
- A series of 11 bis-indolylthiophenes of formula I were obtained by cyclization of bis-indole 1,4-diketones using Lawesson''s reagent. Derivs. I (R = OMe, R1 = SO2Ph), I (R = OMe, R1 = Me), I (R = Cl, R1 = Me), and I (R = OMe, R1 = H) were selected to be evaluated in the full panel of about 60 human tumor cell lines derived from nine human cancer cell types and showed antiproliferative activity generally in the micromolar range. The most sensitive cell lines were: CCRF-CEM, MOLT-4, HL60 (TB), and RPMI-8226 of the leukemia subpanel, HT29 and HCC-2998 cell lines of the colon sub-panel, NCI-H522 of the non-small cell lung cancer sub-panel, LOX IMVI of the melanoma sub-panel, and UO-31 of the renal cancer sub-panel.
- Subjects :
- Cell type
Indoles
cyclization
HL60
Stereochemistry
Clinical Biochemistry
Pharmaceutical Science
Antineoplastic Agents
Thiophenes
Biochemistry
Chemical synthesis
Inhibitory Concentration 50
chemistry.chemical_compound
Alkaloids
5-bis(3'-indolyl)thiophenes
Cell Line, Tumor
Drug Discovery
medicine
Animals
Humans
antitumor activity
Molecular Biology
Cell Proliferation
bis-indolylthiophene
Cell growth
Nortopsentin
Melanoma
Organic Chemistry
Imidazoles
Cancer
Biological activity
DNA
medicine.disease
diketones
Topoisomerase II
DNA Topoisomerases, Type II
chemistry
Cell culture
Molecular Medicine
Subjects
Details
- Language :
- English
- Database :
- OpenAIRE
- Accession number :
- edsair.doi.dedup.....99e05c553553077e26ac153c4406b441