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dc.contributor.authorBai, Ruoli
dc.contributor.authorKazan, Fusun
dc.contributor.authorYagci, Z. Begum
dc.contributor.authorÖZKIRIMLI ÖLMEZ, ELİF
dc.contributor.authorHamel, Ernest
dc.contributor.authorOzkirimli, Sumru
dc.date.accessioned2021-03-05T10:40:12Z
dc.date.available2021-03-05T10:40:12Z
dc.identifier.citationKazan F., Yagci Z. B. , Bai R., ÖZKIRIMLI ÖLMEZ E., Hamel E., Ozkirimli S., "Synthesis and biological evaluation of indole-2-carbohydrazides and thiazolidinyl-indole-2-carboxamides as potent tubulin polymerization inhibitors", COMPUTATIONAL BIOLOGY AND CHEMISTRY, cilt.80, ss.512-523, 2019
dc.identifier.issn1476-9271
dc.identifier.othervv_1032021
dc.identifier.otherav_a45c643a-d0c7-4d9a-b12c-d67d279b0dd9
dc.identifier.urihttp://hdl.handle.net/20.500.12627/109949
dc.identifier.urihttps://doi.org/10.1016/j.compbiolchem.2019.05.002
dc.description.abstractA new series of N'-(substituted phenyl)-5-chloro/iodo-3-phenyl-1H-indole-2-carbohydrazide (5, 6) and N-[2-(substituted phenyl)-4-oxo-1,3-thiazolidin-3-yl]-5-iodo/chloro-3-phenyl-1H-indole-2-carboxamide (7, 8) derivatives were synthesized and evaluated for their anticancer properties. Compounds 5a and 6b, selected as prototypes by the National Cancer Institute for screening against the full panel of 60 human tumor cell lines at a minimum of five concentrations at 10-fold dilutions, demonstrated remarkable antiproliferative activity against leukemia, non-small cell lung cancer, colon cancer, central nervous system (CNS) cancer, melanoma, ovarian cancer, renal cancer, and breast cancer (MCF-7) cell lines with GI(50) values < 0.4 mu M. A subset of the compounds was then tested for their potential to inhibit tubulin polymerization. Compounds 6f and 6g showed significant cytotoxicity at the nM level on MCF-7 cells and exhibited significant inhibitory activity on tubulin assembly and colchicine binding at about the same level as combretastatin A-4. Finally, docking calculations were performed to identify the binding mode of these compounds. Group 5 and 6 compounds interacted with the colchicine binding site through hydrophobic interactions similar to those of colchicine. These compounds with antiproliferative activity at high nanomolar concentration can serve as scaffolds for the design of novel microtubule targeting agents.
dc.language.isoeng
dc.subjectSağlık Bilimleri
dc.subjectTemel Tıp Bilimleri
dc.subjectBiyokimya
dc.subjectTıbbi Biyoloji
dc.subjectBilgisayar Bilimleri
dc.subjectBilgisayar Grafiği
dc.subjectYaşam Bilimleri
dc.subjectTemel Bilimler
dc.subjectMühendislik ve Teknoloji
dc.subjectBİLGİSAYAR BİLİMİ, İNTERDİSİPLİNER UYGULAMALAR
dc.subjectBilgisayar Bilimi
dc.subjectMühendislik, Bilişim ve Teknoloji (ENG)
dc.subjectTıp
dc.subjectYaşam Bilimleri (LIFE)
dc.subjectBiyoloji ve Biyokimya
dc.subjectBİYOLOJİ
dc.titleSynthesis and biological evaluation of indole-2-carbohydrazides and thiazolidinyl-indole-2-carboxamides as potent tubulin polymerization inhibitors
dc.typeMakale
dc.relation.journalCOMPUTATIONAL BIOLOGY AND CHEMISTRY
dc.contributor.departmentİstanbul Üniversitesi , ,
dc.identifier.volume80
dc.identifier.startpage512
dc.identifier.endpage523
dc.contributor.firstauthorID265022


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